382637-45-8Relevant articles and documents
SUBSTITUTED HETEROCYCLIC AMIDE COMPOUND AND PREPARATION METHOD THEREFOR AND PHARMACEUTICAL USE THEREOF
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, (2022/02/02)
Provided are a substituted heterocyclic amide compound having a selective inhibitory effect on RIPK1, and a pharmaceutically acceptable salt, a stereoisomer, a solvate or a prodrug thereof, and a pharmaceutical composition containing the compound, and the
Efficient preparation of (3S)-3-(4-fluorobenzyl)piperidinium mandelate
Emmett, George C.,Cain, Gary A.,Estrella, Melissa J.,Holler, Edd R.,Piecara, James S.,Blum, Andrew M.,Mical, Alfred J.,Teleha, Christopher A.,Wacker, Dean A.
, p. 92 - 96 (2007/10/03)
Methods for the preparation of (3S)-3-(4-fluorobenzyl)piperidine (2) and its mandelate salt (9) are described. The first generation synthesis started from 3-benzylpiperidone, and required Boc protection of the nitrogen for efficient separation of the enantiomers using chromatography on a chiral stationary phase. Subsequently, a resolution method using (R)-mandelic acid, produced high %ee salt 9 after recrystallization and eliminated the need for Boc protection. The third generation route, starting from pyridine-3- carboxaldehyde, led to a streamlined synthesis of racemate 2 and was optimized for producing multi-hundred gram quantities of the chiral salt.
Substituted fused bicyclic amines as modulators of chemokine receptor activity
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Page/Page column 23, (2010/02/13)
The present application describes modulators of CCR3 of formula (Ia) and (Ib): or pharmaceutically acceptable salt forms thereof, wherein Z, R1, R2, R3, R4, R5, R5′, R6, a, b, c, d, and u are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using said modulators are disclosed.