Etilefrine pivalate hydrochloride, K-30052

乙苯福林 匹伐依替福林Chemical Name: DL-(?-alpha-(Ethylaminoethyl)-3'-hydroxybenzyl alcohol 3'-(2,2-dimethylpropionate) hydrochloride; DL-(?-3-(2-Ethylamino-1-hydroxyethyl)phenyl pivalate hydrochloride; 2,2-Dimethylpropanoic acid 3-[2-(ethylamino)-1-hydroxyethyl]phenyl ester hydrochloride
CAS No. 42145-91-5, 709-55-7 (etilefoine), 85750-39-6 (free base)
项目整合开发状态: Phase III
项目研究机构: Fujisawa Deutschland (Originator)
合成路线:3'-Hydroxyacetophenone (I) is acylated with pivaloylchloride (II) to form 3'-pivaloyloxyacetophenone (III).The latter is brominated with bromine to 3'-pivaloyloxy-2-bromoacetophenone (IV),which in turn reacts with N-ethylbenzylamine (V) to form 3'-pivaloyloxy-2-(benzylethylamino)acetophenone (VI).This compound is debenzylated and reduced with H2 in the presence of Pd/C in isopropanol containing hydrochloric acid to yield etilefrine pivalate hydrochloride.