PROCESS FOR PRODUCING 1−H−1,2,4−TRIAZOLE−3−CARBOXYLIC ACID ESTER

Title:

PROCESS FOR PRODUCING 1−H−1,2,4−TRIAZOLE−3−CARBOXYLIC ACID ESTER

Document Type and Number:

WIPO Patent Application WO/2003/042189

Kind Code:

A1

Abstract:

A novel process for producing a 1−H−1,2,4−triazole−3−carboxylic acid ester (compound I−1). The compound (I−1) is obtained by: deaminating 5−amino−1,2,4−triazole−3−carboxylic acid (I−2), halogenating the deaminated acid to obtain an acid chloride, and esterifying it&semi or esterifying the compound (I−2) and then deaminating it&semi or subjecting ethyl−ß−formyloxalylamidrazone to ring closure with the aid of a trialkyl orthoester and an acid. The compound (I−1) is an intermediate for the synthesis of a compound (I−13) (1−(substituted furan)−3−hydroxy−3−(1,2,4−triazole)propenone), which has anti−HIV activity. The process is hence extremely useful.

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Inventors:

SHIMIZU SUMIO (JP)
NISHINO YUTAKA (JP)
YOSHIDA KAZUHIRO (JP)

Application Number:

PCT/JP2002/011981

Publication Date:

May 22, 2003

Filing Date:

November 15, 2002

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Assignee:

SHIONOGI & CO (JP)
SHIMIZU SUMIO (JP)
NISHINO YUTAKA (JP)
YOSHIDA KAZUHIRO (JP)

International Classes:

C07D249/10; C07D249/14; (IPC1-7): C07D249/10; C07D249/14; C07D405/06

Domestic Patent References:

WO2000039086A1

2000-07-06

Foreign References:

US4639266A	1987-01-27
DE4225778A1	1994-02-17

Attorney, Agent or Firm:

Yamamoto, Shusaku (15th Floor 2-27, Shiromi 1-chome, Chuo-k, Osaka-shi Osaka, JP)

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