J. Appl. Cryst.の発刊に際して

10. Patented Literature 2616 10.1. Esterification 2616 10.2. Ether Formation 2619 10.2.1. Etherification without Cyclization 2619 10.2.2. Etherification with Cyclization 2624 10.3. N-Alkylation 2625 10.4. Other Reactions 2627 11. Summary and Outlook 2628 12. Note Added in Proof 2628 13. Abbreviations Used in This Review 2629 14. Acknowledgments 2629 15. Supporting Information Available 2630 16. References 2630

Mitsunobu and Related Reactions: Advances and Applications

The Complementary Competitors: Palladium and Copper in C-N Cross-Coupling Reactions

Green synthesis of silver nanoparticles using Alternanthera dentata leaf extract at room temperature and their antimicrobial activity

Cover -- Advancesin Heterocyclic Chemistry13; -- Copyright Page -- Contents -- Contributors -- Preface13; -- Chapter 113; Hexameric Macrocyclic Architectures in Heterocyclic Chemistry -- 1. Introduction -- 2. Macrocycles with Five-Membered Heterocyclic Subunits -- 3. Six-Membered Ring Heterocycles -- 4. Miscellaneous Heterocyclic Materials -- 5. Conclusions -- References -- Chapter 2 13;Metal-Catalyzed Intramolecular Heteroatom (X)!Carbon(C) Functional Group Migration Reactions Involving Additionsof X2;Y Bonds Across Alkynes -- 1. Introduction -- 2. Synthesis of O-Containing Heterocycles -- 3. Synthesis of N-Containing Heterocycles -- 4. Synthesis of S-Containing Heterocycles -- 5. Synthesis of Se-Containing Heterocycles -- 6. Conclusions -- Acknowledgments -- References -- Chapter 313; Biindolyls -- 1. Introduction -- 2. Synthesis -- 3. Reactions -- 4. Conclusion -- References -- Chapter 413; The Annulation of 2-Imidazolines -- 1. Introduction -- 2. Polar Annulation Strategy -- 3. Imidazolines as Double Nucleophiles -- 4. Annulations of the Enamino Ester/Ketene Aminal -- 5. Annulations of N-Unsubstituted 2-Imidazolines -- 6. Imidazolines as Sources of 1,3-Dipoles -- 7. Azomethine Ylides by Alkylation2;Deprotonation -- 8. Azomethine Ylides by Carbene Insertion in a Catalytic Cycle -- 9. Azomethine Ylides by Conjugate Addition-Proton Transfer -- 10. Annulations Using Chiral Imidazolines -- 11. Optically Active Piperidines via Enamino Ester Annulation -- 12. Dipolar Cycloaddition of Optically Active Imidazolinium Ylides -- 13. Chiral Imidazoline Nitrones in Cycloadditions -- 14. Summary -- References -- Chapter 5 Recent Advances in the Dimroth Rearrangement: A ValuableTool for the Synthesis of Heterocycles -- 1. Introduction -- 2. Translocation of Heteroatoms in Fused Heterocycles (Type 1) -- 3. Translocation of Exo- and Endocyclic Heteroatoms in Heterocycles(Type 2) -- Acknowledgments -- References -- Subject Index.

Advances in Heterocyclic Chemistry

Developing early-maturing and stress-resistant potato varieties

The potato processing industry requires cultivars with high tuber dry matter and acceptable colour of processed products. Hence an attempt was made to find out the extent of heterosis, type and nature of gene action and the suitable parents for tuber dry matter, yield, tuber number and average tuber weight. Fourteen parents and their 40 progenies from factorial (10 x 4) mating design were evaluated for two clonal generations. Data were recorded and subjected to heterosis and combining ability analyses. In general, progenies were better than mid parent value for number of tubers, lower for average tuber weight and as good as for yield and dry matter. Mean squares due to various sources including interactions with generations were significant for all the characters. Both additive and non-additive gene actions were equally important for various characters. Specific combining ability effects of crosses were related to general combining ability effects of the parents involved. Use of at least one parent with good general combining ability resulted in high-performing heterotic progenies for various characters. Superior parents and hybrids for yield and dry matter were also identified.

Heterosis and combining ability for tuber dry matter and yield in potato (Solatium tuberosum L.) over two clonal generations under short-day sub-tropic conditions

An efficient and facile one-pot synthesis of 1,3-disubstituted isoquinolines 3 was accomplished from 3-substituted isocoumarins 1 through diketones, formed in situ via the Grignard reaction, in the presence of ammonium acetate, montmorillonite K-10 catalyst, and ethanol solvent. R = Phenyl, 4-chlorophenyl, 4-methylphenyl R′ = phenyl, methyl, isopropyl, cyclopentyl, cyclohexyl, 3-methoxyphenyl, 2,4-dichlorphenyl,benzyl, biphenyl, 4-pyridyl
 .

Facile benzannulation of isocoumarins in the efficient synthesis of diversified 1,3-disubstituted isoquinolines

Thyroxine, the main secretory hormone of thyroid gland, is produced from thyroglobulin by thyroid peroxidase/hydrogen peroxide/iodide system. The prohormone T4 is then converted to its potent form T3 by a selenocysteine-containing enzyme iodothyronine deiodinase. Autoantibodies which activate thyroid-stimulating hormone receptor are not under the pituitary feedback control system, and therefore, the uncontrolled production of thyroid hormones leads to a condition called “hyperthyroidism.” The overproduction of T4 and T3 can be controlled by specific inhibitors, which either block the synthesis of thyroid hormone or reduce the conversion of T4–T3. Unique classes of such inhibitors are thiourea drugs, methimazole (MMI), 6-n-propyl-2-thiouracil, and carbimazole suggesting that thione moiety exhibit excellent antithyroid activity. We have carried out biomimetic studies by HPLC assay, which suggested that isochromene-1-thiones exhibit significant antithyroid activity by inhibiting the lactoperoxidase (LPO)-catalyzed iodination, comparable with MMI, and that the inhibitory effects of some of them were found to be much superior to those of MMI. Kinetic studies demonstrate that isochromene-1-thiones inhibit LPO irreversibly. Our inhibition studies suggest that isochromene-1-thiones might be another promising candidate with potential for developing therapeutics for hyperthyroidism. The quantitative structure–activity relationship (QSAR) was developed between the LPO-inhibitory activities of isochromene-1-thiones and their physiochemical properties. The statistical measures, such as r2 (0.81), r2adj (0.79), q2 (0.73), and F-ratio (39.05), were found to be within the acceptable range.

Antithyroid agents and QSAR studies: inhibition of lactoperoxidase-catalyzed iodination reaction by isochromene-1-thiones

The title compound, C15H13N3, contains two independent mol­ecules in the asymmetric unit. The isoquinoline moiety and phenyl rings form dihedral angles of 4.38 (2) and 10.14 (3)° in the two independent mol­ecules. The crystal packing is stabilized by N—H⋯N mol­ecular dimers formed across a center of symmetry.

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P. Manivel

Papers

Developing early-maturing and stress-resistant potato varieties

Heterosis and combining ability for tuber dry matter and yield in potato (Solatium tuberosum L.) over two clonal generations under short-day sub-tropic conditions

Facile benzannulation of isocoumarins in the efficient synthesis of diversified 1,3-disubstituted isoquinolines

Antithyroid agents and QSAR studies: inhibition of lactoperoxidase-catalyzed iodination reaction by isochromene-1-thiones

1-(3-Phenyl-isoquinolin-1-yl)hydrazine.