Global Patent Index - EP 1003902 A1

EP 1003902 A1 20000531 - METHOD FOR RACEMIC BIOCHEMICAL RESOLUTION OF CIS- AND TRANS- PYRROLOPIPERIDINE

Title (en)

METHOD FOR RACEMIC BIOCHEMICAL RESOLUTION OF CIS- AND TRANS- PYRROLOPIPERIDINE

Title (de)

VERFAHREN ZUR RACEMATSPALTUNG VON CIS- UND TRANS- PYRROLOPIPERIDIN

Title (fr)

PROCEDE POUR LE DEDOUBLEMENT RACEMIQUE DE CIS- ET TRANS- PYRROLOPIPERIDINE

Publication

EP 1003902 A1 20000531 (DE)

Application

EP 98943821 A 19980801

Priority

  • DE 19735198 A 19970814
  • EP 9804820 W 19980801

Abstract (en)

[origin: DE19735198A1] Optical resolution of a racemic cis- or trans-pyrrolo-piperidine derivative of formula (I) involves: (a) enzymatically mono-acylating a mixture containing (R,R)- and (S,S)-(I) or (S,R)- and (R,S)-(I) to give a mixture containing (R,R)- and (S,S)-6-acyl-(I) or (S,R)- and (R,S)-6-acyl-(I); (b) further enzymatically acylating to give a mixture containing (S,S)-1,6-diacyl- and (R,R)-6-acyl-(I) or (S,R)-1,6-diacyl- and (R,S)-6-acyl-(I); (c) removing the enzyme and optionally solvent and excess acylating agent; (d) treating the residue with aqueous acid; (e) separating (S,S)-1,6-diacyl-(I) or (S,R)-1,6-diacyl-(I) by extraction; (f) making the extraction residue alkaline; and (g) separating (R,R)-6-acyl-(I) or (R,S)-1,6-diacyl-(I) by extraction. Also claimed are: (i) mixtures containing (R,R)- and (S,S)-6-acyl-(I); (ii) (S,S)-1,6-diacyl-(I); (iii) (R,R)-6-acyl-(I); and (iv) (R,R)-1,6-diacyl-(I).

IPC 1-7

C12P 41/00; C12P 17/18; C07D 471/04

IPC 8 full level

C07D 471/04 (2006.01); C12P 17/18 (2006.01); C12P 41/00 (2006.01)

CPC (source: EP KR US)

C07D 471/04 (2013.01 - EP US); C12P 17/182 (2013.01 - EP US); C12P 41/00 (2013.01 - KR); C12P 41/007 (2013.01 - EP US)

Designated contracting state (EPC)

AT BE CH DE ES FI FR GB IE IT LI NL PT SE

DOCDB simple family (publication)

US 6153414 A 20001128; AU 9158098 A 19990308; CA 2300119 A1 19990225; CN 1267334 A 20000920; DE 19735198 A1 19990218; EP 1003902 A1 20000531; HU 0004660 A2 20010428; HU 0004660 A3 20040428; IL 134169 A0 20010430; JP 2001514901 A 20010918; KR 20010022843 A 20010326; WO 9909200 A1 19990225

DOCDB simple family (application)

US 48508300 A 20000203; AU 9158098 A 19980801; CA 2300119 A 19980801; CN 98808155 A 19980801; DE 19735198 A 19970814; EP 9804820 W 19980801; EP 98943821 A 19980801; HU 0004660 A 19980801; IL 13416998 A 19980801; JP 2000509862 A 19980801; KR 20007001445 A 20000212