Compounds of formula (I):
or a pharmaceutically acceptable salt, ester or amide thereof, wherein:
Ar is benzofuran-2-yl, or phenyl optionally substituted by groups R' and/or R2 wherein R' is halogen, trifluoromethyl or hydroxy and R2 is halogen;
R3 is hvdrogen or methyl;
Xis-
in which
a is an integer from 1 to 6,
b is an integer from 2 to 7,
M is hydroxy, C1-6 alkoxy, phenyl C1-6 alkoxy, or-NR4 R5 in which R4 and R5 are each hydrogen or C1-6 alkyl or together form a five or six membered heterocyclic ring;
Y is C2-6 straight or branched alkylene, with at least two carbon atoms between the -O- and -OH; and n is 1 or 2, having anti-obesity and/or anti-hyperglycaemic activity, pro- cessesfortheir preparation and their pharmaceutical use.
式(I)化合物:
或其药学上可接受的盐、酯或酰胺,其中
Ar 是苯并呋喃-2-基,或任选被基团 R' 和/或 R2 取代的苯基,其中 R' 是卤素、三氟甲基或羟基,R2 是卤素;
R3 是氢或甲基;
Xis-
其中
a 是 1 到 6 的整数、
b 是 2 至 7 的整数、
M 是羟基、C1-6 烷氧基、C1-6 烷氧基苯基或-NR4 R5,其中 R4 和 R5 各自是氢或 C1-6 烷基,或共同形成一个五或六个成员的杂环;
Y 是 C2-6 直链或支链亚烷基,在-O-和-OH 之间至少有两个碳原子;以及 n 是 1 或 2,具有抗肥胖和/或抗高血糖活性、制备方法及其药物用途。
US4692465A
申请人:——
公开号:US4692465A
公开(公告)日:1987-09-08
Phosphonium salts and aldehydes from the convenient, anhydrous reaction of aryl acetals and triphenylphosphine hydrobromide
作者:Mani Ramanathan、Duen-Ren Hou
DOI:10.3998/ark.5550190.0014.308
日期:——
The reactions of aryl acetals/ketals and triphenylphosphine hydrobromide gave the corresponding aldehydes/ketones and alkyl phosphonium bromides. This reaction was applied to convert acetals/ketals to the corresponding aldehydes/ketones under an anhydrous and convenient condition (50 oC, 5 min, up to 90% yield), and acid sensitive functional groups were compatible.