Topic
Substituent
About: Substituent is a research topic. Over the lifetime, 42877 publications have been published within this topic receiving 516716 citations. The topic is also known as: side chain & side group.
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01 Oct 1997TL;DR: In this article, novel 4-aminoquinazoline derivatives of the formula (See formula I) were disclosed. But they are not suitable for the treatment of hyperproliferative disorders and conditions in mammals.
Abstract: Disclosed are novel 4-aminoquinazoline derivatives of the formula (See formula I) (wherein Z is NR3R4 in which R3 is H and R4 is Q2 or phenyl substituted with (R5)q or Z is (See formula II) the dotted line represents an optional double bond; R5 is a substituent such as halo, amino, alkyl, alkoxy, etc.; R6 is a substituent such as hydroxyl, amino, sulfo, alkoxy, carboxyl, etc.; q is 0-3; o is 0-2; Q2 is a 9- or 10-membered bicyclic heterocyclic moiety; Q1 is Ar-Y-X in which Ar is mono- or bicyclic (hetero)aryl, X is alkenylene, alkynylene or bond and Y is (CH2)p where p is 0-5; R1 is a substituent such as trifluoromethyl; n is 0-3; m is 1-2) and their pharmaceutically acceptable salts. Those compounds and the salts are useful for the treatment of hyperproliferative disorders and conditions in mammals.
201 citations
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TL;DR: This new N-heterocyclic carbene precursor bearing fluorine substitution in the backbone results in significantly improved enantioselectivities across a range of substrates.
Abstract: The catalytic asymmetric intermolecular Stetter reaction of heterocyclic aldehydes and nitroalkenes has been developed. We have identified a strong stereoelectronic effect on catalyst structure when a fluorine substituent is placed in the backbone. X-ray structure analysis provides evidence that hyperconjugative effects are responsible for a change in conformation in the azolium precatalyst. This new N-heterocyclic carbene precursor bearing fluorine substitution in the backbone results in significantly improved enantioselectivities across a range of substrates.
198 citations
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198 citations
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198 citations