[EN] PROCESS FOR PREPARING METHYL PHENIDATE HYDROCHLORIDE<br/>[FR] PROCÉDÉ DE PRÉPARATION DE CHLORHYDRATE DE PHÉNIDATE DE MÉTHYLE
申请人:HARMAN FINOCHEM LTD
公开号:WO2011067783A1
公开(公告)日:2011-06-09
Disclosed herein is a process for the preparation of methyl phenidate hydrochloride (Formula I), comprising the steps of; hydrolyzing α-phenyl-α-pipyridyl acetamide (Formula II) in presence of mineral acid at reflux temperature and subsequent neutralization to yield threo -α-phenyl-α-pipyridyl-2-acetic acid (Formula III) which in presence of acidic catalyst reacts with methanol followed by treatment with alcoholic hydrochloride solution produces methyl phenidate hydrochloride.
Synthesis of β-Hydroxy α-Amino Acids Through Brønsted Base-Catalyzed <i>syn</i>-Selective Direct Aldol Reaction of Schiff Bases of Glycine <i>o</i>-Nitroanilide
作者:Silvia Vera、Ana Vázquez、Ricardo Rodriguez、Sandra del Pozo、Iñaki Urruzuno、Abel de Cózar、Antonia Mielgo、Claudio Palomo
DOI:10.1021/acs.joc.1c00406
日期:2021.6.4
Here we report the highly enantio- and syn-selective synthesis of β-hydroxy α-amino acids from glycine imine derivatives under Brønsted base (BB) catalysis. The key of this approach is the use of benzophenone-derived imine of glycine o-nitroanilide as a pronucleophile, where the o-nitroanilide framework provides an efficient hydrogen-bonding platform that accounts for nucleophile reactivity and diastereoselectivity