Global patent index - EP 1003902 A1

EP 1003902 A1 2000-05-31 - 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 (DE)

Application

EP 98943821 A

Priority

  • DE 19735198 A
  • EP 9804820 W

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 (main, further and additional classification)

C12P 41/00; C07D 471/04; C12P 17/18

IPC 8 full level (invention and additional information)

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

CPC (invention and additional information)

C07D 471/04 (2013.01); C12P 17/182 (2013.01); C12P 41/007 (2013.01)

Citation (search report)

See references of WO 9909200A1

Designated contracting state (EPC)

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

EPO simple patent family

DE 19735198 A1 19990218; AU 9158098 A 19990308; CA 2300119 A1 19990225; CN 1267334 A 20000920; EP 1003902 A1 20000531; HU 0004660 A2 20010428; HU 0004660 A3 20040428; IL 134169 D0 20010430; JP 2001514901 A 20010918; US 6153414 A 20001128; WO 9909200 A1 19990225

INPADOC legal status

2003-03-05 [18W] WITHDRAWN

- Ref Legal Event Code: 18W

- Effective date: 20030113

2000-05-31 [17P] REQUEST FOR EXAMINATION FILED

- Ref Legal Event Code: 17P

- Effective date: 20000314

2000-05-31 [AK] DESIGNATED CONTRACTING STATES:

- Ref Legal Event Code: AK

- Designated State(s): AT BE CH DE ES FI FR GB IE IT LI NL PT SE