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Process for the synthesis of (3S, 4S) - Tetrahydrofuran - 3 - 4 - isopropyl - - il 6,7 Dihydro 3h imidazo [4,5-c] pyridine - (4H) - carboxylate
专利权人:
PROXIMAGEN LIMITED
发明人:
申请号:
ARP170102966
公开号:
AR109883A1
申请日:
2017.10.25
申请国别(地区):
AR
年份:
2019
代理人:
摘要:
The application relates to an improved process for the synthesis of (3S, 4S) - Tetrahydrofuran - 3 - 4 - isopropyl - - il 6,7 Dihydro 3h imidazo [4,5-c] pyridine - (4H) - carboxylateAnd pharmaceutically acceptable salts thereof, such as methanesulfonic acid salt, and intermediaries.Claim 1, a process for the preparation of (3S, 4S) - Tetrahydrofuran - 3 - 4 - isopropyl - - il 6,7 Dihydro 3h imidazo [4,5 - C] pyridine - (4H) - carboxylate and pharmaceutically acceptable salts thereof, characterized in that it comprises the step of converting a Histamine reaction formula (1) in 4 - isopropyl - 4,5,6,7 - tetrahydro - 3h imidazo [4,5-c] pyridine of formula (2), which includes isobutiraldehído reaction stage.In the Reaction is kept at a temperature of between 50 and 100 C for a period of 1 to 12 hours.Claim 10: 4 - isopropyl - - 4,5,6,7 tetrahydro - 3h imidazo [4,5-c] pyridine dihydrochloride characterized because it is obtained from a process according to claim 7.Claim 14: a process for the preparation of (3S, 4S) - Tetrahydrofuran - 3 - 4 - isopropyl - - il 6,7 Dihydro 3h imidazo [4,5 - C] pyridine - (4H) - carboxylate and pharmaceutically acceptable salts thereof, which comprises the step of coupling reaction of 4 - isopropyl - - 4,5,6,7 tetrahydro - 3h imidazo [4,5 - C] pyridine of formula (2) and (S) - (+) - 3 - hidroxitetrahidrofurano formula (3) using a coupling Agent to form (3S) - tetrahydrofuran-3-yl 4 - isopropyl - 6.7 - dihydro 3h imidazo [4,5 - C] pyridine - (4H) - carboxylate of formula (4), wherein the coupling Agent is n, N - disuccinimidil carbonate.Claim: 19 (3S) - tetrahydrofuran-3-yl 4 - isopropyl - 6.7 - dihydro 3h imidazo [4,5 - C] pyridine - 5 - (4H) - carboxylate wherein is obtained from a process according to any one of Claims 14 to 16.Claim 20: a Preparation Process of (3S, 4S) - Tetrahydrofuran - 3 - 4 - isopropyl - - il 6,7 Dihydro 3h imidazo [4,5 - C] pyridine - (4H) - carboxylate and pharmaceutically acceptable salts thereof, characterized i
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