Showing papers by "Roussel Uclaf published in 1971"
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TL;DR: The interaction of estradiol and testosterone with rat plasma proteins has been studied by equilibrium dialysis, sucrose gradient centrifugation, column chromatography and polyacrylamide gel electrophoresis, finding that Estradiol Binding Plasma Protein, unlike several synthetic estrogens, is bound with greater affinity, whereas non estrogenic steroids including testosterone are not bound at all.
242 citations
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TL;DR: In this article, a computer program is presented which permits the calculation of the geometries and corresponding energies of any molecule which can be submitted to treatment by the strain energy minimization method.
49 citations
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22 Mar 1971TL;DR: In this article, the authors proposed a framework for PREPARING PENTACYCLIC ALKLOIDS of General FormulA: 12-(CH3-OOC-),12-HO,13A-(CH 3-CH2-)-1,2,5,6,12,13-3H- INDOLO(3, 2,1-DE)PYRIDO (3,2.1-IJ)(1,5)NAPHTHYRIDINE
Abstract: PROCESS FOR PREPARING PENTACYCLIC ALKLOIDS OF GENERAL FORMULA: 12-(CH3-OOC-),12-HO,13A-(CH3-CH2-)-1,2,5,6,12,13-3H- INDOLO(3,2,1-DE)PYRIDO(3,2,1-IJ)(1,5)NAPHTHYRIDINE
21 citations
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20 citations
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03 Feb 1971TL;DR: In this article, the authors presented a scheme to select a group of HYDROGEN, ALKYL, and HYDROXY ALKHYML of 1 to 5 CARBON ATOMS.
Abstract: NOVEL CONDENSED CYCLIC THIO COMPOUNDS OF THE FORMULA 1-(R-OOC-CH2-),3,4-(-(CH2)N-S-)BENZENE WHEREIN N IS AN INTEGER FROM 2 TO 4 AND R IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, ALKYL AND HYDROXY ALKYL OF 1 TO 5 CARBON ATOMS AND NON-TOXIC, PHARMACEUTICALLY ACCEPATABLE METAL SALTS AND NITROGEN BASE SALTS HAVING ANALGESIC, ANTI-INFLAMMATORRY AND ANTI-PYRETIC ACTIVITY AND THEIR PREPARATION.
19 citations
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28 Apr 1971TL;DR: NOVEL ALKYL 3-(3'' - OR - TRANS 1''-ALKENYL)-CYCLOPENTANONE-2-CARBOXYLates of the FormulA 2-(ALK-OOC-),3-(CH3-( CH2)M-CH(-O-R)-CH=CH-)CYclopentan-1- One wherein ALK is ALkyl OF 1 TO 7 CARBON ATOMS, R is SELECTED from the group CONSISTING of HYDROGEN, ACYL OF
Abstract: NOVEL ALKYL 3-(3'' - OR - TRANS 1''-ALKENYL)-CYCLOPENTANONE-2-CARBOXYLATES OF THE FORMULA 2-(ALK-OOC-),3-(CH3-(CH2)M-CH(-O-R)-CH=CH-)CYCLOPENTAN-1- ONE WHEREIN ALK IS ALKYL OF 1 TO 7 CARBON ATOMS, R IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, ACYL OF AN ORGANIC CARBOXYLIC ACID OF 1 TO 18 CARBON ATOMS AND A-TETRAHYDROPYRANYL AND M IS 3, 4 OR 5 WHICH ARE INTERMEDIATES FOR PROSTAGLANDINS AND THEIR PREPARATION AND NOVEL INTERMEDIATES.
10 citations
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28 Dec 1971TL;DR: In this paper, a new procedure of preparation of EBURNAMONINE of the formula: 12-(O=),13A-(CH3-CH2-)-2,3,4A,5,6,12,13, 13,13A-OCTAHYDRO- 1H-INDOLO(3,2,1-DE)PYRIDO(1,5)NAPHTHYRIDINE
Abstract: THE OBJECT OF THIS INVENTION IS A NEW PROCESS OF PREPARATION OF ($) EBURNAMONINE OF THE FORMULA: 12-(O=),13A-(CH3-CH2-)-2,3,4A,5,6,12,13,13A-OCTAHYDRO- 1H-INDOLO(3,2,1-DE)PYRIDO(3,2,1-IJ)(1,5)NAPHTHYRIDINE IT IS KNOWN THAT EBURANAMONINE HAS BEEN ISOLATED FROM SEVERAL PLANT SPECIES SUCH AS VINCA MINOR AND HUNTERIA EBURNEA. EBURNAMONINE POSSESSES INTERESTING PHARMACOLOGICAL PROPERIES, IT PROVOKES A HYPERTENSION ACCOMPANIED BY A RESPIRATORY AND CARDIAC STIMULATION AND AN INCREASE OF TONICITY. IN ADDITION, EBURNAMONINE CAN SERVE AS STARTING MATERIAL IN THE SYNTHESIS OF KNOWN ANALOGOUS COMPOUNDS DISPLAYING AN INTERESTING PHYSIOLOGICAL ACTIVITY.
7 citations
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02 Feb 1971TL;DR: In this article, an impulse modulator including a charging capacitor, a voltage comparator, a constant current generator and first and second modulating voltage sources is presented, and two modulators may be combined in an anticoincidence circuit to make the combined modulator output strictly proportional to the ratio of the first modulating voltages.
Abstract: An impulse modulator including a monostable multivibrator having a charging capacitor, a voltage comparator, a constant current generator and first and second modulating voltage sources. The voltage comparator insures that the multivibrator rapidly changes from its astable state to its stable state, and the duration of the astable period is proportional to the ratio of the first modulating voltage, and a constant voltage, to a second modulating voltage. Two modulators may be combined in an anticoincidence circuit to make the combined modulator output strictly proportional to the ratio of the first and second modulating voltages.
6 citations
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21 Jan 1971TL;DR: In this paper, a member is selected from the group consisting of HYDROXY, ALKOXY of 1 to 4 CARBON ATOMS, CYCLOALKOXY of 5 to 6 CARBOM ATOMs, and ACYLOXY, where the ACYL is derived from an ORGANIC CARBOXYLIC ACID HAVING 1 TO 10 CARBOOMS.
Abstract: NOVEL 11B-LOWER ALKOXY-$1,3,5(10)-GONATRIENS SUBSTITUTED IN THE 3-POSITIONS BY A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROXY, ALKOXY OF 1 TO 4 CARBON ATOMS, CYCLOALKOXY OF 5 TO 6 CARBOM ATOMS, AND ACYLOXY, WHEREIN THE ACYL IS DERIVED FROM AN ORGANIC CARBOXYLIC ACID HAVING 1 TO 10 CARBOM ATOMS, IN THE 13-POSITION BY A LOWER ALKYL RADICAL, AND IN THE 17-POSITION BY THE GROUPING (X-O-),(Y--) WHEREIN X IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND ALKYL OF 1 TO 4 CARBON ATOMS, AND Y IS SELECTED FROM THE GROUP CONSISTING OF A HYDROCARBON RADICAL AND A SUBSTITUTED HYDROCARBON RADICAL. THESE COMPOUNDS POSSESS ESTROGENIC ACTIVITY.
5 citations
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06 Jul 1971TL;DR: In this article, the group consisting of hydrogen and lower alkyl having excellent pesticidal properties and their preparation is selected from the groups consisting of a hydrogen and a lower alkkyl.
Abstract: WHEREIN R and R1 may be different and are lower alkyl and R2 is selected from the group consisting of hydrogen and lower alkyl having excellent pesticidal properties and their preparation. Substituted oximes of the formula
5 citations
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08 Oct 1971TL;DR: In this paper, the formulae 1-(2-R-PHENYL), 2-R,2 -R1,5-X'',6-X-BENZIMIDAZOLE wherein X and X'' may be DIFFERENT and are selected from the group CONSISTING of HYDROGEN, HALOGEN and ALKYL, ALKOXY, TRIHALOMETHYL and NITRO, R is SELECTED from the Group Consisting of -COOH-, -COOR'', and
Abstract: BENZIMIDAZOLES OF THE FORMULA 1-(2-R-PHENYL),2-R1,5-X'',6-X-BENZIMIDAZOLE WHEREIN X AND X'' MAY BE DIFFERENT AND ARE SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, HALOGEN, ALKYL, ALKOXY, TRIHALOMETHYL AND NITRO, R IS SELECTED FROM THE GROUP CONSISTING OF -COOH-, -COOR'', AND -CO-N(-A)-B R'' IS SELECTED FROM THE GROUP CONSISTING OF ALIPHATIC AND HYDROXYLATED RESIDUE OF A GLYCOL, A AND B ARE SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND OPTIONALLY SUBSTITUTED ALIPHATIC AND R1 IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, LOWER ALIPHATIC HYDROCARBON, UNSUBSTITUTED AND POLYSUBSTITUTED ARYL, ARYLALIPHATIC, A THIENYL, A B-PYRIDYL AND A FURYL WITH THE PROVISO THAT WHEN R1 IS PHENYL, X'' AND X ARE OTHER THAN HALOGEN, ALKOXY AND TRIFLUOROMETHYL WHICH COMPOUNDS POSSESS ANTI-INFLAMMATORY AND ANTIVIRAL ACTIVITY AND A NOVEL PROCESS FOR THEIR PREPARATION.
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26 Jan 1971TL;DR: In this article, at least one leader was selected from a group consisting of homologists of ACRAMIDE and METHACRYLAMIDE, COPOLYMERS OF ACRAMEY and ACRYLIC ACID, and COPOYSMERS of METH ACRIMEY and CARAMIDE to provide methods of treating or pre-venting ULCERS or inflaming large-scale aggression in WARM-BLOODED ANIMALS.
Abstract: DIGESTIVE TRACT PROTECTING COMPOSITIONS CONTAINING AS THE ACTIVE INGREDIENT AT LEAST ONE POLYMER SELECTED FROM THE GROUP CONSISTING OF HOMOPOLYMERS OF ACRYLAMIDE AND METHACRYLAMIDE, COPOLYMERS OF ACRYLAMIDE AND ACRYLIC ACID AND COPOLYMERS OF METHACRYLAMIDE AND METHACRYLIC ACID AND TO METHODS OF TREATING OR PREVENTING ULCERS OR INFLAMMATION OF LARGE INTESTINE IN WARM-BLOODED ANIMALS.
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04 Oct 1971TL;DR: Gonadienes of the 12-X,13-R,17-(R1=)-GONA-4,9,11-TRIEN-3-ONE and 12-ALKYL:$4.9.
Abstract: NOVEL 12B-ALKYL-$4.9-GONADIENES OF THE FORMULA 12-X,13-R,17-(R1=)-GONA-4,9-DIEN-3-ONE AND 12-ALKYL:$4.9.11-GONATREIENES OF THE FORMULA 12-X,13-R,17-(R1=)-GONA-4,9,11-TRIEN-3-ONE WHEREIN R IS ALKYL OF 1 TO 3 CARBON ATOMS, X IS ALKYL OF 1 TO 3 CARBON ATOMS AND R1 IS SELECTED FROM THE GROUP CONSISTING OF (R2-O-),(H-); (R2-O-),(R3-); AND (HO-),(R3-) WHEREIN R2 IS SELECTED FROM THE GROUP CONSISTING OF HYDROCARBYL OF 1 TO 10 CARBON ATOMS AND ACYL OF AN ORGANIC CARBOXYLIC ACID OF 1 TO 18 CARBON ATOMS AND R3 IS SELECTED FROM THE GROUP CONSISTING OF SATURATED HYDROCARBON OF 1 TO 6 CARBON ATOMS AND UNSATURATED HYDROCARBON OF 2 TO 6 CARBON ATOMS WHICH COMPOUNDS POSESS HORMONAL PROPERTIES AND TO TWO NOVEL PROCESSES FOR THEIR PREPARATION AND NOVEL INTERMEDIATES THEREFOR.
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04 Oct 1971TL;DR: In this article, a process for the preparation of analogs of VITAMIN B12 is described, where a HYDROCARBON RADICAL R is attached to the COBALT ATOM by reacting to a CO-Z COBAMIDE where Z is an ANION-FORMING group with a METALLIC OR METALLOID DERIVATIVE of R.
Abstract: A PROCESS FOR THE PREPARATION OF ANALOGS OF VITAMIN B12 WHEREIN A HYDROCARBON RADICAL R IS ATTACHED TO THE COBALT ATOM BY REACTING A CO-Z COBAMIDE WHEREIN Z IS AN ANION-FORMING GROUP WITH A METALLIC OR METALLOID DERIVATIVE OF R.
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03 Feb 1971TL;DR: In this paper, the 2,2-dimethyl steroids of the formula STR1 were selected from the group consisting of hydrogen, --OH and STR2 and the dotted line in the B ring indicated the optional presence of a double bond in the 6(7) position.
Abstract: Novel 2,2-dimethyl steroids of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, --OH and ##STR2## R 1 is selected from the group consisting of hydrogen and hydrocarbon of 1 to 17 carbon atoms Z is selected from the group consisting of hydrogen and ##STR3## in the α-position, R 2 is alkyl of 1 to 4 carbon atoms and the dotted line in the B ring indicates the optional presence of a double bond in the 6(7) position having antialdosterone activity and increasing sodium diuresis while conserving organic potassium.
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06 Jan 1971TL;DR: In this paper, the authors present a comparison of different approaches for treating MICROBIC INFECTIONS in warm-blooded animals using N-SUCCINYL-GLUTAMIC ACID and its non-toXIC, PHARMACEUTICALLY ACCEPTABLE SALTS with MINERAL OR ORGANIC bases.
Abstract: COMPOSITIONS FOR TREATING MICROBIC INFECTIONS HAVING AS THE ACTIVE INGREDIENT RACEMIC OR OPTICALLY ACTIVE ISOMERS OF N-SUCCINYL-GLUTAMIC ACID AND ITS NON-TOXIC, PHARMACEUTICALLY ACCEPTABLE SALTS WITH MINERAL OR ORGANIC BASES AND A METHOD OF COMBATTING INFECTIONS IN WARM-BLOODED ANIMALS.
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28 Oct 1971TL;DR: A COMPOUND SELECTED from the Group Consisting of ACETAMIDES of the FormulA CH*C-CH2-C(-C6H5)2-CO-N(-R)-CH(-R1)-CH 2-N(R2)-R2-R3)-R3 wherein R is selected from the group CONISTING of HYDROGEN and ALKYL of 1 TO 4 CARBON ATOMS, R1 is HYDRogen, R2 is Alkyl, R3 is ARYL and
Abstract: A COMPOUND SELECTED FROM THE GROUP CONSISTING OF ACETAMIDES OF THE FORMULA CH*C-CH2-C(-C6H5)2-CO-N(-R)-CH(-R1)-CH2-N(-R2)-R3 WHEREIN R IS SELECTED FROM THE GROUP CONISTING OF HYDROGEN AND ALKYL OF 1 TO 4 CARBON ATOMS, R1 IS HYDROGEN, R2 IS ALKYL OF 1 TO 4 CARBON ATOMS AND R3 IS SELECTED FROM THE GROUP CONSISTING OF ALKYL OF 1 TO 4 CARBON ATOMS, ARYL AND ARALKYL OR THE GROUP -N<(-CH2-CH2-N(-)-R2-R-) MAY FORM A 6-MEMBERED NITROGEN-CONTAINING HETEROCYCLIC OR THE GROUP -CH<(-CH2-N(-)-R2-R1-) MAY FROM A 6-MEMBERED NITROGEN-CONTAINING HETEROCYCLIC OR THE GROUP -N(-R2-R3-) MAY FORM A 5- TO 6-MEMBERED, NITROGEN-CONTAINING HETEROCYCLIC OPTIONALLY CONTAINING ANOTHER HETERO-ATOM AND THEIR NON-TOXIC, PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS WHICH HAVE INTENSE ANALGESIC ACTIVITY AND ACT AS POTENTIALIZERS FOR NEURO-SEDATIVES AND THEIR PREPARATION AND INTERMEDIATES THEREOF.
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30 Aug 1971TL;DR: In this article, a novel process for the preparation of derivatives of prostanoic acids of the prostaglandin A 2 (PGA 2 ) group of the formula ##STR1## was proposed.
Abstract: A novel process for the preparation of derivatives of prostanoic acids of the prostaglandin A 2 (PGA 2 ) group of the formula ##STR1## wherein R is selected from the group consisting of hydrogen and lower alkyl, n is a whole number of 2, 3 or 4 and m is a whole number of 3, 4 or 5 and to novel intermediates produced in the said process.
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07 Jul 1971TL;DR: In this article, the 4-amino-quinolines of the formula where R is selected from the group consisting of hydrogen, halogen, -CF3, lower alkyl, lower alkoxy, upper alkylsulfonyloxy, lower arabinosynthetic aryl and lower acylamino, R1 is selected, R2 and Q are selected, and X is selected.
Abstract: Novel 4-amino-quinolines of the formula WHEREIN R is selected from the group consisting of hydrogen, halogen, -CF3, lower alkyl, lower alkoxy, lower alkylsulfonyloxy, lower alkylthio, nitro, lower alkylamino, lower acylamino and cyano, R1 is selected from the group consisting of hydrogen, chlorine and methyl, Y is selected from the group consisting of 2,3 and 3,4-disubstituted thiophenes of the formula AND 4,5 DISUBSTITUTED THIAZOLES OF THE FORMULA WHEREIN R2 and Q are selected from the group consisting of hydrogen and lower alkyl and X is selected from the group consisting of hydrogen, lower alkyl, a phenyl, diloweralkylamino lower alkylene, N-morpholino lower alkylene, Z , R3 and R4 being hydrogen and taken together form P and P1 are lower alkyl, P2 is selected from the group consisting of lower alkyl and monocyclic aryl, M and M' are lower alkyl, Z is halogen and n is an integer from 1 to 6, and their non-toxic, pharmaceutically acceptable acid addition salts having analgesic and anti-inflammatory activity and their preparation. Lower alkyl means having 1 to 6 carbon atoms.
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28 Sep 1971TL;DR: An amide of 2-hydroxy-3-methoxy-5-allyl-benzoic acid of the formula WHEREIN R is selected from the group consisting of hydrogen, alkyl of 1 to 7 carbon atoms and acyl of an organic carboxylic acid of 1-18 carbon atoms, R1 and R2 taken together with the nitrogen atom form a heterocyclic which may contain another heteroatom, which products possess outstanding choleretic properties far superior to dehydrocholic acid as mentioned in this paper.
Abstract: An amide of 2-hydroxy-3-methoxy-5-allyl-benzoic acid of the formula WHEREIN R is selected from the group consisting of hydrogen, alkyl of 1 to 7 carbon atoms and acyl of an organic carboxylic acid of 1 to 18 carbon atoms, R1 and R2 taken together with the nitrogen atom form a heterocyclic which may contain another heteroatom, which products possess outstanding choleretic properties far superior to dehydrocholic acid. D R A W I N G
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03 Feb 1971TL;DR: In this article, a group consisting of HYDROGEN, ACYL of an ORGANIC CARBOXY-LIC ACID of 1 to 18 CARBON ATOMS, LOWER ALIPHATIC, ARALYALIPHATEIC and HETEROCYCLIC WHICH have ANIT-AND-ROGENIC ACTIVITY, their PREPARATION, their INTERMEDIATE, their pre-paration and INTERMEDIA, their neighbors thereFROM.
Abstract: NOVEL 11B,18-EPOXY-$4.9-ESTRADIENES OF THE FORMULA 3-(O=),11,18-(-O-),17-R,17-(R''-O-)ESTRA-4,9-DIENE WHEREIN R IS SELECTED FROM THE GROUPS CONSISTING OF HYDROGEN AND ETHYNYL AND R'' IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, ACYL OF AN ORGANIC CARBOXYLIC ACID OF 1 TO 18 CARBON ATOMS, LOWER ALIPHATIC, ARALYALIPHATIC AND HETEROCYCLIC WHICH HAVE ANIT-ANDROGENIC ACTIVITY, THEIR PREPARATION AND INTERMEDIATES THEREFROM.
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09 Jun 1971•
19 Feb 1971TL;DR: In this article, the authors present a PHARMACEUTICAL COMPOSITION for the control of acute or chronic colchic diarrhea, which consists of a minimum and a major amount of a PULVERULENT, PHARCARGE-GRADE POLYAMIDE.
Abstract: THE PRESENT INVENTION RELATES TO A PHARMACEUTICAL COMPOSITION FOR THE CONTROL OF ACUTE OR CHRONIC DIARRHEA WHICH COMPRISES A MINOR AMOUNT OF A PULVERULENT, PHARMACEUTICAL-GRADE POLYAMIDE SELECTED FROM THE GROUP CONSISTING OF NYLON 6, NYLON 66, NYLON 610, NYLON 11 AND COPOLYMERS OF NYLON 66 AND NYLON 12 AND A MAJOR AMOUNT OF A PHARMACEUTICAL MEDIUM. THE PHARMACEUTICAL COMPOSITION IS UTILIZED FOR CONTROLLING DIARRHEA BY ORALLY ADMINISTERING THE COMPOSITION CONTAINING A THERAPEUTICALLY EFFECTIVE AMOUNT OF THE ACTIVE PRINCIPLE TO A SUBJECT SUFFERING FROM DIARRHEA.
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29 Dec 1971TL;DR: A Novel Process for the Preparation of TRIENIC SteroIDS of the Formula 3-(O=),17-HO,17-X,17 X,13-RESTRA-4,9,11-TRIENE as discussed by the authors.
Abstract: A NOVEL PROCESS FOR THE PREPARATION OF TRIENIC STEROIDS OF THE FORMULA 3-(O=),17-HO,17-X,13-R-ESTRA-4,9,11-TRIENE WHEREIN R IS ALKYL OF 1 TO 4 CARBON ATOMS AND X IS SELECTED FROM THE GROUP CONSISTING OF ALIPHATIC OF 1 TO 6 CARBON ATOMS OPTIONALLY SUBSTITUTED AND CYCLOALKYL OF 3 TO 6 CARBON ATOMS AND TO NOVEL INTERMEDIATES FOR THE SAID PROCESS.
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TL;DR: A method of healing wounds in the skin of warm-blooded animals which comprises applying to such a wound an effective amount of 17 Beta -acetoxy-Delta 4,9,11.
Abstract: A method of healing wounds in the skin of warm-blooded animals which comprises applying to such a wound an effective amount of 17 Beta -acetoxy- Delta 4,9,11
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10 Nov 1971TL;DR: A semi-stereospecific process for the preparation of alkyl 3,11-dimethyl-7-ethyl-2,6,10-tridecatrienoate is described in this paper.
Abstract: A novel process for the preparation of alkyl 3,11-dimethyl-7-ethyl-2,6,10-tridecatrienoate wherein alkyl is a hydrocarbon of one to five carbon atoms in a semi-stereospecific manner which are useful intermediates for the preparation of juvenile hormone and to novel intermediates therefor.