Benzo(b)thiophen-5-yl derivative and process for producing the same,申请号ZA19930002493-传众专利搜索

Benzo(b)thiophen-5-yl derivative and process for producing the same

申请公布号：ZA9302493(B)

申请号：ZA19930002493

申请日期：1993.04.07

申请公布日期：1993.11.12

申请人：

TOYAMA CHEMICAL CO. LTD.

发明人：JOJI NAKANO;NOBUHISA TAYA;HISAAKI CHAKI;TETSUO YAMAFUJI;KAISHU MOMONOI

分类号：C07D333/58;C07D;C07D409/04

主分类号：C07D333/58

摘要：Prodn.of an optically active benzo(b)thiophen-5-yl dialkylamino-ethoxy-ethanol deriv., of formula (VIA), (VIB) or their salts, comprising: (a) inoculating a supersatd. soln. of a dioxolo of formula (I) with seed crystals of the optically active dioxolo (IIA) or (IIB), depending on whether (VIA) or (VIB) is the objective, in the presence of a racemisation catalyst, to crystallise optically active (IIA) or (IIB) preferentially; (b) subjecting to alcoholysis or hydrolysis in presence of an acid catalyst; (c) protecting the free OH gp. to give (IIIA) or (IIIB); (d) reducing to diol deriv. (IVA) or (IVB); (e) reacting with a dialkylaminoethyl halide of formula (V); and (f) removal of the OH protecting gp., if desired, is new. In the formulae, R2 = H or a protecting gp.; R4,R5 = 1-6C alkyl; R2a = a protecting gp.; R3 = H or a protecting gp.; and BT = benzo(b)thiophen-5-yl; and X = a removable gp.. Specifically claimed are cpds. (-)-1-(Benzo(b)thiophenyl -5-yl)-2-(2- (N,N-diethylamino) ethoxy)ethanol; and (-) or (+) 2,2-dimethyl-(benzo(b)thiophen-5-yl)- 1,3-dioxolan-4-one.