Bosutinib Methanoate synthesis

Yield:-

Reaction Conditions:

in methanol at 65; for 0.5 h;

Steps:

7

EXAMPLE 7: Preparation of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4- methyl-l-piperazinyl)propoxy]-3-quinolinecarbonitrile, Form VI. [0068] 4-[(2,4-Dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-l- piperazinyl)propoxy]-3-quinolinecarbonitrile (10 g) and 200 mL of methanol were heated to 65⁰C and held with stirring for 30 minutes. The hot mixture was cooled to room temperature and filtered. The material obtained was washed with 80 mL MeOH and dried in vacuo to give 8.31 g of 4-[(2,4-dichloro-5- methoxyphenyl)amino]-6-methoxy-7- [3 -(4-methyl- 1 -piperazinyl)propoxy] -3 - quinolinecarbonitrile methanolate Form VI by XRD scans.

References:

WO2007/5462,2007,A1 Location in patent:Page/Page column 18