新产品编号:1226559

Chemical Name:
项目整合开发状态:
项目研究机构:
合成路线:The optical resolution of 1-benzylazetidine-2-carboxamide (I) with L-tartaric acid in the usual way gave 1-benzylaetidine-2(R)-carboxamide (II),which is reduced with borane-THF complex yielding 2(R)-(aminomethyl)-1-benzylazetidine (III).The debenzylation of (III) with H2 over Pd/C in ethanol affords 2(R)-(aminomethyl)azetidine (IV),which is finally condensed with 5-amino-1-cyclopropyl-6,7,8-trifluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (V) by means of 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) in hot pyridine.