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EP0220601A1 Expired / Lapsed EP ⏱️ 0.0 years remaining

Pyranoindolizine derivatives and preparation process thereof

Assignee: Daiichi Pharmaceutical Co Ltd
•
Filing: 1986-10-14
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Granted: —
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Expires: 2006-10-14
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Abstract

Abstract A pyranoindolizine derivative represented by the following general formula (I): wherein R means a hydrogen atom or hydroxyl group and Q denotes with a proviso that Q is other than C=O when R is a hydrogen atom. Its preparation process is also described.

Inventors

  • 👤 Hiroaki c/o Daiichi Seiyaku Res.Inst. Tagawa
  • 👤 Hirofumi c/o Daiichi Seiyaku Res.Inst. Terasawa
  • 👤 Akio c/o Daiichi Seiyaku Res.Inst. Ejima

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-28 09:22
CPC Classifications
C; C07; C07D; C07D493/00; C07D493/12; C07D493/14

Claims Analysis

Total Claims: 9
Claim 1
Independent Claim 41 words
I. A pyranoindolizine derivative represented by the following general formula (I): wherein R means a hydrogen atom or hydroxyl group and Q denotes with a proviso that Q is other than  C = 0 when R is a hydrogen atom.
Claim 2
Dependent Claim 9 words
A pyranoindolizine derivative represented by the following formula (I*b):
Claim 3
Dependent Claim 9 words
A pyranoindolizine derivative represented by the following formula (I*c):
Claim 4
Dependent Claim 32 words
A process for the preparation of a pyranoindolizine derivative represented by the following formula - (Ia): which comprises subjecting a compound represented by the following formula (V): to a ring closing reaction.
Claim 5
Dependent Claim 26 words
A process for the preparation of a pyranoindolizine derivative represented by the following formula :-(lb) which comprises oxidizing a compound represented by the following formula (Ia):
Claim 6
Dependent Claim 31 words
A process for the preparation of a pyranoindolizine derivative represented by the following formula - (Ic): which comprises subjecting a compound represented by the following formula (Ib): to a deketalizing reaction.
Claim 7
Dependent Claim 70 words
A process for the preparation of a pyranoindolizine derivative represented by the following formula - (I*c): which comprises reacting (R)-(+)-α-methyl-benzylamine or (S)-(-)-a-methyl-benzylamine with a compound represented by the following formula (Ib): to form a compound represented by the following formula (VIII) or (IX): isolating from the compound (VIII) or (IX) a diastereomer represented by the following formula (VI) or (VII): and then subjecting the diastereomer to a ring closing reaction.
Claim 8
Dependent Claim 136 words
A process for the preparation of a pyranoindolizine derivative represented by the following formula - (I*b): which comprises halogenating a compound represented by the following formula (X): to obtain a compound represented by the following formula (Xl): wherein X means a halogen atom, causing (R)-N-tosylproline or an alkali metal salt thereof to act on the compound (XI) to form a compound represented by the following formula (XII): wherein Ts means a tosyl group, ethylating the compound (XII) to form a compound represented by the following formula (XIII): reducing the compound (XIII) to obtain a compound represented by the following formula (XIV): subjecting the compound (XIV) to a transfer reaction in the presence of a nitrosating agent to form a compound represented by the following formula: and then subjecting the compound (XV) to a ring closing reaction.
Claim 9
Dependent Claim 35 words
An intermediate suitable for use in the preparation of a pyranoindolizine derivative, said intermediate being represented by the following formula: wherein R means a cyano, acetylaminomethyl or acetoxymethyl group and Ts denotes a tosyl group.

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