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1,2-Benzisoxazole derivatives

1,2-Benzisoxazole derivatives. Naruto, Shunsuke; Kadokawa, Toshiaki; Kawashima, Katzuyoshi (Dainippon Pharmaceutical Co., Ltd.In this study， 13444-24-1 and 100-35-6 are also used. , Japan). Eur. Pat. Appl. EP 94833 A2 23 Nov 1983, 41 pp. DESIGNATED STATES: R: DE, FR, GB, IT. (English). (European Patent Organization). CODEN: EPXXDW. CLASS: IC: C07D261-20; C07D413-12; A61K031-41; A61K031-445. APPLICATION: EP 83-302789 17 May 1983. PRIORITY: JP 82-84501 18 May 1982. DOCUMENT TYPE: Patent CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Section cross-reference(s): 1, 63 Benzisoxazoleacetate esters I (R = H, halo, OH, alkyl, CF3, alkoxy; R1 = OH, CH2OH, cycloalkyl, OPh, SPh, CH2Ph; R2 = H, CH2Ph; R3 = N,N-disubstituted aminoalkyl, cyclic aminoalkyl, such as 1-methyl-4-piperidinyl) were prepd., and they showed antispasmodic activity stronger than that of rociverine. I (R = R1 = R2 = H, R3 = Me) was converted to I (R = R2 = R3 = H, R1 = cyclohexyl), and the latter was treated with Et2N(CH2)3OH, 4-MeC6H4SO2Cl, and Et3N to give I [R = R2 = H, R1 = cyclohexyl, R3 = (CH2)3NEt2]. .

1,2-Benzisoxazole derivatives

1,2-Benzisoxazole derivatives. Adachi, Ikuo; Ueda, Motohiko; Kimoto, Sadatoshi (Shionogi and Co., Ltd., Japan). Japan. Kokai JP 52031070 9 Mar 1977 Showa, 6 pp. (Japanese). (Japan). CODEN: JKXXAF. CLASS: IC: C07D261-20.Chemical with cas number 65476-09-7 also plays role. PRIORITY: GB 75-36296 3 Sep 1975. DOCUMENT TYPE: Patent CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Seventeen title derivs. I [R = H, Cl, Me, AcNH, MeO, PhCH2O; R1 = H, Me, MeO; R2 = H; R1 and R2 may be bound to form CH:CHCH:CH; R3 = iso-Pr, tert-Bu, 3,4-(MeO)2C6H3CH2CH2] were prepd., e.g., by reaction of II with epihalohydrins followed by reaction of the resulting epoxides with R3NH2. Thus, reaction of II (R = R1 = R2 = H) with epibromohydrin gave 3-(2,3-epoxypropoxy)-1,2-benzisoxazole, which (4 mmol) in MeOH was autoclaved with 2 mL iso-PrNH2 4 h at 85° to give I (R = R1 = R2 = H, R3 = iso-Pr) (yield not given). The b-acceptor blocking data of I (R = R1 = R2 = H, R3 = tert-Bu) (III) were given using isolated guinea pig tracheas and hearts in comparison with propranolol; LD50 of III was 38.3 mg/kg (i. 65476-09-7 is the cas registry number. This chemical is also mentioned in this article.v.) in mice. ..