Reference

Hydrogenated isoquinolines and their peripheral vascular disease treating compositions

Hydrogenated isoquinolines and their peripheral vascular disease treating compositions. Le Polles, Jean Bernard; Martin, Michel; Nadler, Guy; Saias, Edmond (Laboratoires Sobio S. A., Fr.). U.S. US 4442108 A 10 Apr 1984, 7 pp. Cont. of U.S. Ser. No. 196,322, abandoned.In this experiment, several chemicals are used like 61381-04-2 (English). (United States of America). CODEN: USXXAM. CLASS: IC: C07D215-14; A61K031-47. NCL: 424258000. APPLICATION: US 81-300957 10 Sep 1981. PRIORITY: US 78-898145 20 Apr 1978; US 80-196322 14 Oct 1980. DOCUMENT TYPE: Patent CA Section: 31 (Alkaloids) Section cross-reference(s): 1, 63 Isoquinolines I (R 1 R1 = alkoxy, R2 = R3 = H, R2R3 = bond) and their hydrochlorides were prepd. Thus, 3,4-(EtO)2C6H3CH2CH2NH2 was treated with 3,4-(Me2CHO)2C6H3CH2CO2Et to give 3,4-(Me2CHO)2C6H3CH2CONHCH2CH2C6H3(OEt)2-3,4, which was cyclized to give I.HCl (R = Et, R1 = CHMe2; R2R3 = bond). The latter compd. at 1.1 ′ 10-5 mol/L inhibited 50% of the BaCl2-induced contractions of isolated guinea pig ileum, compared with 9.8 ′ 10-4 mol/L for papaverine.HCl. It caused transient hypotension accompanied by a decrease in the amplitude of ventricular contraction. .