N-(2-AMINO-4,6-DICHLOROPYRIMIDINE-5-YL)FORMAMIDE AND PRODUCTION OF THE SAME

Title:

N-(2-AMINO-4,6-DICHLOROPYRIMIDINE-5-YL)FORMAMIDE AND PRODUCTION OF THE SAME

Document Type and Number:

Japanese Patent JP3811966

Kind Code:

B2

Abstract:

PURPOSE: To obtain a new pyrimidine derivative capable of being converted into corresponding nucleotide in a high yield without difficulties.
CONSTITUTION: The derivative is N-(2-amino -4,6-dichloropyrimidine -5-yl) formamide of formula I. The derivative is obtained by cyclyzing an aminomalonic ester of formula II (R1 is an 1 to 6C alkyl or its salt) with guanidine or its salt in the presence of a base to produce 2,5-diamino-4,6- dihydroxypyrimidine or its salt of formula III, chlorinating this product with chlorinating agent in the presence of an amide of the formula IV (R5 is a 5 to 6-membered heterocycloalkyl, etc.), to produce 4,6-dichloropyrimidine of the formula V (R5 is -NH2), and reacting the compound with an aqueous solution of a carboxylic acid to produce the subject compounds.

Inventors:

Gerhard Stucky
Rene im Winkelried

Application Number:

JP10149995A

Publication Date:

August 23, 2006

Filing Date:

April 25, 1995

Export Citation:

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Assignee:

LONZA LIMITED

International Classes:

A61K31/70; C07D239/48; A61P31/12; (IPC1-7): C07D239/48; //A61K31/70

Domestic Patent References:

JP9508412A

Attorney, Agent or Firm:

Sooo Suga

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