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US5036153A Expired / Lapsed US ⏱️ 0.0 years remaining

Preparation of 2,5-diazabicyclo[2.2.1]heptanes and intermediates

Assignee: Pfizer Inc
•
Filing: 1989-10-18
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Granted: 1991-07-30
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Expires: 2009-10-18
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Abstract

Abstract Diazabicyclo[2.2.1]heptane intermediates are prepared from 4-hydroxy-L-proline in a five step procedure, or from allo-4-hydroxy-D-proline, through a novel 2-(C1-c6)alkyl-5-substituted-2,5-diazabicyclo[2.2.1]heptane intermediate. The diazabicycloheptanes are of use in the preparation of antibiotic quinolones.

Inventors

  • 👤 Tamim F. Braish
  • 👤 Darrell E. Fox

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-01 05:49
CPC Classifications
C; C07; C07D; C07D487/00; C07D487/02; C07D487/08; A; A61; A61P; A61P31/00; A61P31/04; C07D207/00; C07D207/46; C07D207/48; C07D487/06

Claims Analysis

Total Claims: 3
Claim 1
Independent Claim 82 words
A process for preparing a compound of the formula ##STR16## wherein X is SO 2 or CO 2 , and R 2 is C 1 -C 6 alkyl, trifluoromethyl, benzyl, or phenyl or phenyl substituted by one or two C 1 -C 6 alkyl, halogen, nitro, methoxy, or trifluoromethyl, which comprises heating a compound of the formula ##STR17## wherein X and R 2 are as defined above, with tosylchloride in pyridine at a temperature of about 70 ° to about 115° C.
Claim 2
Dependent Claim 82 words
A process for preparing a compound of the formula ##STR16## wherein X is SO 2 or CO 2 , and R 2 is C 1 -C 6 alkyl, trifluoromethyl, benzyl, or phenyl or phenyl substituted by one or two C 1 -C 6 alkyl, halogen, nitro, methoxy, or trifluoromethyl, which comprises heating a compound of the formula ##STR17## wherein X and R 2 are as defined above, with tosylchloride in pyridine at a temperature of about 70 ° to about 115° C.
Claim 3
Dependent Claim 16 words
A process according to claim 1 wherein X is SO 2 and R 2 is p-tolyl.

References Cited (Backward Citations)

US3083208A Cited
US3459768A Cited
US3905979A Cited
US3947445A Cited
GB2102801A Cited
DE3302697A1 Cited
JPS60190760A Cited
US4861779A Cited
JPS63162672A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1994-07-29 1995-01-28 1995-07-30 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1998-07-29 1999-01-28 1999-07-30 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2002-07-29 2003-01-28 2003-07-30 $7700.00 Window Closed / Lapsed

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