Stereospecific hydrolysis of optically active esters
申请人:——
公开号:US20030032818A1
公开(公告)日:2003-02-13
1
A new, more efficient and highly stereospecific process is described for the preparation of compounds with general formula (R)-(I) and of absolute configuration (R), where the groups M, W, Q and Q
1
are as defined in the description, starting from compounds of absolute configuration (S) by hydrolysis, in the presence of acids, of the corresponding esterified derivatives. The (R)-(I) products obtained with the process described herein are chiral synthons useful for the production of enanthiomerically pure drugs. The preparation of (R)-carnitine is also provided.
Process for the preparation of 3-amino-pyrrolidine derivatives
申请人:F. Hoffmann-La Roche AG
公开号:EP0928787A1
公开(公告)日:1999-07-14
The invention is concerned with a process for the manufacture of 3-amino-pyrrolidine derivatives of the formula
wherein
R1signifies hydrogen, alkyl, cyclo-alkyl, alkenyl, aryl or an amino protecting group; and
R2, R3each independently signify hydrogen, alkyl, cyclo-alkyl, alkenyl or aryl;
by converting a compound of the formula
wherein
Xsignifies a protected hydroxy group;
in the presence of a primary amine of the formula R1NH2 into the pyrrolidine derivative of the formula
wherein X and R1 have the aforementioned significances;
which is subsequently reacted in the presence of R2R3NH under pressure; and with the use of this process for the production of vinylpyrrolidinone-cephalosporin derivatives.