PEMIROLAST synthesis

3synthesis methods

Product Name:PEMIROLAST
CAS Number:69372-19-6
Molecular formula:C10H8N6O
Molecular Weight:228.21

4-Imino-9-methyl-4H-pyrido[1,2-a]pyrimidine-3-carbonitrile

102781-19-1
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69372-19-6
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Yield: 75%

Reaction Conditions:

with hydrogenchloride;acetic acid

Steps:

9 EXAMPLE 9
EXAMPLE 9 To 60 ml of acetic acid were added 10.0 g (54.3 mmoles) of 3-cyano-4-imino-9-methyl-4H-pyrido[1,2-a]pyrimidine and 3.53 g (54.3 mmoles) of sodium azide, and the reaction was carried out with stirring at 115° C. for 1 hour. Then, 15 ml of concentrated hydrochloric acid was added and the resulting mixture was subjected to reaction with stirring at 100° C. for 2 hours. After cooling, the crystals precipitated were collected by filtration to obtain 9.1 g of light-brown powder of 9-methyl-3-(1H-tetrazol-5-yl)-4H-pyrido[1,2-a]pyrimidin-4-one. Yield: 75%. M.p. 281° C. (decomp.).

References:

Wako Pure Chemical Industries, Ltd.;Tokyo, Tanabe Co., Ltd. US5081243, 1992, A