Methanesulfonic acid salt of pyrazolopyrimidine compound,...

C - Chemistry – Metallurgy – 07 – D

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C07D 487/04 (2006.01) A61K 9/08 (2006.01) A61K 31/519 (2006.01) A61K 47/10 (2006.01) A61P 1/00 (2006.01) A61P 5/04 (2006.01) A61P 5/10 (2006.01) A61P 15/00 (2006.01) A61P 25/00 (2006.01) A61P 29/00 (2006.01) A61P 37/00 (2006.01) C07C 253/30 (2006.01) C07C 255/40 (2006.01)

Patent

CA 2529561

8-(3-Pentylamino)-2-methyl-3-(2-chloro-4-methoxy~phenyl)-6,7-dihydro-5H- cyclopenta[d]pyrazolo[1,5-a]~pyrimidine methanesulfonate, which is novel, and a process for producing an intermediate for the compound. 8-(3-Pentylamino)-2- methyl-3-(2-chloro-4-methoxy~phenyl)-6,7-dihydro-5H-cyclopenta[d]pyrazolo[1,5- a]~pyrimidine methanesulfonate is a compound having highly excellent thermal stability. The novel production process enables a compound represented by the general formula (I): (I) (wherein Ar represents an optionally substituted benzene ring, etc.; and R1 represents C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, etc.), which is an intermediate, to be efficiently produced in a high yield.

La présente invention concerne un noveau composé, le 8-(3-pentylamino)-2-méthyl-3-(2-chloro-4-méthoxy-phényl)-6,7-dihydro-5H-cyclopenta[d]pyrazolo[1,5-a]-pyrimidine méthanesulfonate. L'invention concerne également un procédé de production d'un intermédiaire permettant l'obtention du composé de l'invention. En l'occurrence, le 8-(3-pentylamino)-2-méthyl-3-(2-chloro-4-méthoxy-phényl)-6,7-dihydro-5H-cyclopenta[d]pyrazolo[1,5-a]-pyrimidine méthanesulfonate est un composé présentant un niveau supérieur de stabilité thermique. Le procédé de production de l'invention permet un rendement élevé de production d'un composé intermédiaire représenté par la formule générale (I). Dans cette formule, Ar est un noyau benzène éventuellement substitué, et R?1¿ est C¿1-8? alkyle, C¿2-8? alcényle, C¿2-8? alkynyle, etc.

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