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【结 构 式】 
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【药物名称】Safinamide mesilate, FCE-28073(R-isomer), PNU-151774E, NW-1015, FCE-26743 【化学名称】2(S)-[4-(3-Fluorobenzyloxy)benzylamino]propionamide methanesulfonate 【CA登记号】202825-46-5, 133865-89-1 (free base) 【 分 子 式 】C18H23FN2O5S 【 分 子 量 】398.45681 |
【开发单位】Newron (Originator) 【药理作用】Antiepileptic Drugs, Antiparkinsonian Drugs, Cerebrovascular Diseases, Treatment of, Extrapyramidal Disorders, Treatment of, NEUROLOGIC DRUGS, Stroke, Treatment of, Calcium Channel Modulators, Dopamine Reuptake Inhibitors, MAO-B Inhibitors, Sodium Channel Blockers |
合成路线1
Safinamide has been obtained by reductocondensation of 4-(3-fluorobenzyloxy)benzaldehyde (I) with L-alaninamide (II) by means of sodium cyanoborohydride in methanol.
| 【1】 Sorbera, L.A.; Castaner, J.; Leeson, P.A.; Safinamide mesilate. Drugs Fut 2001, 26, 8, 745. |
| 【2】 Bonsignori, A.; Pevarello, P.; Dostert, P.; et al.; Synthesis and anticonvulsant activity of a new class of 2-[arylalkyl)amino]alkanamide derivatives. J Med Chem 1998, 41, 4, 579. |
| 【3】 Dostert, P.; Pevarello, P.; Heidempergher, F.; Varasi, M.; Bonsignori, A.; Roncucci, R. (Pharmacia Corp.); N-Phenylalkyl substd. alpha-amino carboxamide derivs. and process for their preparation. EP 0400495; EP 0426816; JP 1992500215; US 5236957; US 5391577; US 5502079; WO 9014334 . |
| 【4】 Dostert, P.; Pevarello, P.; Bonsignori, A.; Varasi, M.; Synthesis and anticonvulsant activity of new benzyloxybenzylacetamide derivatives. 12th Int Symp Med Chem (Sept 13-17, Basel) 1992, Abst P-089.C. |
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