NEW MATERIAL:The 3,5-disubstituted-1,2,4-oxadiazole derivative of formula I (R is lower alkyl, lower alkenyl, aryl or heterocyclic group; X is CO, CH2, CH2O, single bond, etc.; Y is H, halogen, OH, etc.; T is single bond, lower alkylene, etc.; U is H, lower alkyl, lower alkenyl, lower alkoxy-lower alkyl, lower alkoxycarbonyl-lower alkyl, etc.; Z is O, S, etc.). EXAMPLE:5-(3-Fluoro-4-phenyl-alpha-methylbenzyl)-3-ethylsulfonyl-1,2,4 -oxadiazole. USE:It has anti-inflammatory activity, and useful as a remedy for inflammation diseases such as rheumatoid arthritis, osteoarthritis, lumbago, etc. Free from side effects such as digestive tract disorder. PREPARATION:The compound of formula I can be prepared e.g. by reacting the acylisothiocyanate derivative of formula II with the compound of formula III(Uz is lower alkyl, etc.; Z1 is O, etc.), reacting the reaction product with the compound of formula IV, and further reacting with hydroxylamine.
展开▼
机译：新材料：式I的3,5-二取代-1,2,4-恶二唑衍生物（R为低级烷基，低级烯基，芳基或杂环基; X为CO，CH2，CH2O，单键等; Y是H，卤素，OH等; T是单键，低级亚烷基等; U是H，低级烷基，低级烯基，低级烷氧基-低级烷基，低级烷氧基羰基-低级烷基等; Z是O， S等）。实施例：5-（3-氟-4-苯基-α-甲基苄基）-3-乙基磺酰基-1,2,4-恶二唑。用途：具有抗炎作用，可作为类风湿性关节炎，骨关节炎，腰痛等炎症疾病的治疗药物。无消化道疾病等副作用。制备：可以制备例如式I的化合物。通过使式II的酰基异硫氰酸酯衍生物与式III的化合物反应（Uz为低级烷基等; Z 1为O等），使反应产物与式IV的化合物反应，并进一步与羟胺反应。
展开▼
