3760-52-9Relevant articles and documents
Heterocyclization and Spirocyclization Processes Based on Domino Reactions of N-Tosylhydrazones and Boronic Acids Involving Intramolecular Allylborylations of Nitriles
Plaza, Manuel,Parisotto, Stefano,Valdés, Carlos
supporting information, p. 14836 - 14843 (2018/09/25)
Polycyclic molecules featuring all-carbon quaternary bridgehead centers were synthesized through domino cyclizations between N-tosylhydrazones and boronic acids. Variations of the general cascade have been applied for the preparation of 3-quinuclidinones and related alkaloid-like scaffolds through transannular heterocyclizations. Moreover, the employment of 3-cyanopropyl and 4-cyanobutylboronic acids and α,β-unsaturated N-tosylhydrazones led to spirocycles through unprecedented formal [n+1] cyclizations, including the stereoselective spirocyclization of the Hajos–Parrish ketone. The common feature of all the new reactions described is the creation of an all-carbon quaternary center by formation of two Csp3?C bonds on the hydrazonic carbon atom. DFT-based calculations suggested the occurrence of cascade processes, which involve a diazo compound carboborylation followed by a 1,3-borotropic rearrangement on an intermediate allylboronic acid and a novel bora-aza-ene cyclization.
PYRAZOL DERIVATIVES
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Page/Page column 14, (2009/02/11)
The invention is concerned with novel pyrazol derivatives of formula (I), wherein R1, R2, R3, R4, X and Y are as defined herein, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR-2 receptor and/or CCR-5 receptor and can be used as medicaments.
Oxime derivatives
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, (2008/06/13)
An oxime derivative of the formula: STR1 wherein R is a hydrogen atom or a C1-5 alkyl group, R1 is a hydrogen atom, a C1-5 alkyl group or a carboxyl-protecting group, R2 is a hydrogen atom, a halogen atom, a hydroxyl group or an amino group, R3 is a C3-7 cycloalkyl group, R4 is a hydrogen atom, a halogen atom or a C1-4 alkoxy group, each of R5 and R6 which may be the same or different, is a hydrogen atom or a C1-5 alkyl group, or R5 and R6 together represent a C2-4 alkylene group which forms together with the adjacent carbon atom a C3-5 ring, provided that when R2 is a hydrogen atom, R4 is a C1-4 alkoxy group, m is an integer of 0 or 1, and n is an integer of from 1 to 3; or its pharmaceutically acceptable salt.