Synthesis Of Benzoxazole- And Benzothiazole-based ROCK Inhibitors

A wide variety of protein kinases are widely distributed in human body. T hese kinases are take part in various kinds of life activities and play a very i mportant role in treatment of dieases. In these protein kinases, Rho kinase (RO CK) as an important target for treating many disease, such as cardiovascular a nd cerebrovascular diseases, nervous system diseases and cancer which is a ver y important member, has become a hot topic of research. This paper mainly d oes the following two aspects of work.(1)Optimized the synthesis route of benzoxazole ROCK inhibitor SR4148. Improve the shortcomings of synthesis route which trifluoroacetic acid salt will open ring in DMSO, increase the prtity of product of benzoxazole ROCK inh ibitor SR4148. And ues the improved method, synthesis 10mg benzoxazole RO CK inhibitors SR4148.(2)Through studies the methodology of construct the benzothiazole ring, us e the smelly and environment-friendly thiourea as the S source and optimized t he synthetic route, the route only two steps can synthesis benzothiazole derivati ves circulately from benzene acetamide derivatives, which saves the cost. Using this method to synthetize benzothiazole ROCK inhibitors SR6494, to achieve t he economic, efficient and environmental protection.