PRODUCTION OF 2'-PYRROLIDINEPROPANOIC ACID DERIVATIVE

Title:

PRODUCTION OF 2'-PYRROLIDINEPROPANOIC ACID DERIVATIVE

Document Type and Number:

Japanese Patent JPH10251227

Kind Code:

A

Abstract:

To industrially advantageously obtain the subject compound by treating a new N-protected-2-prolinal as a starting raw material with periodic acid.

An N-protected 2-prolinal of formula I (R1 is an amino-protecting group, preferably tert-butoxycarbonyl group; R2 is a lower alkyl, preferably methyl) in an amount of 1mol is treated with at least 1mol of periodic acid in an inert solvent (tetrahydrofuran) at -20 to 50°C to give the objective compound of formula II which is one of important raw materials for synthesizing dorastatin 10, etc., having antitumor action. The compound of formula II is a new compound and is usually obtained by reacting 1mol of the compound of formula III with at least about 1mol of a compound of formula IV in an inert solvent in the presence of a base (lithium diisopropylamide) at -100 to 0°C.

Inventors:

GONDO MASAAKI
MIYAZAKI KOICHI
SUGIMURA AKIHIRO
ITO TAKESHI
KOURA YUJI

Application Number:

JP6752497A

Publication Date:

September 22, 1998

Filing Date:

March 06, 1997

Export Citation:

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Assignee:

TEIKOKU HORMONE MFG CO LTD

International Classes:

C07D207/08; (IPC1-7): C07D207/08

Attorney, Agent or Firm:

Heiyoshi Odashima (1 person outside)

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