水素化ホウ素ナトリウム-遷移金属塩系による有機化合物の還元(第3報) : 2-Aminomethyl-1,1-diphenyl-1-buteneの製造

概要

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Preparative methods for 2-aminomethyl-1,1-diphenyl-1-butene (I), a hypertensive drug, were investigated. The following three-step method was suggested to be the most suitable for the preparation of I. The first process is to obtain 2-cyano-1,1-diphenyl-1-butanol (II) by condensation of butyronitrile and benzophenone in the presense of sodium hydride (molar ratio, 1 : 2 : 2) at 90°. The second is the reduction of II by sodium borohydride-CoCl_2 system (molar ratio, II : NaBH_4 : CoCl_2=1 : 10 : 2) in MeOH at 20° to 2-aminomethyl-1,1-diphenyl-1-butanol (III), and the final step is the dehydration of III to I in a mixture of acetic acid and conc. hydrochloric acid (20 : 1).
公益社団法人日本薬学会の論文
1970-12-25