公开(公告)号：US5008411A

公开(公告)日：1991-04-16

申请号：US416295

申请日：1989-10-02

申请人： David L. Coffen ,  Pradeep B. Madan ,  Alan Schwartz

发明人： David L. Coffen ,  Pradeep B. Madan ,  Alan Schwartz

IPC分类号： C07C319/20 ,  C07C323/56 ,  C07D281/08 ,  C07D281/10

CPC分类号： C07C319/20 ,  C07D281/08 ,  C07D281/10 ,  C07C2101/14

摘要： A process for the preparing a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are each independently hydrogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen, trifluoromethyl or nitro; or R.sub.1 and R.sub.2 taken together with the benzene ring to which they are attached are naphthalene, and Ar is p-lower alkoxy phenyl.which comprises reacting ##STR2## wherein R.sub.1 and R.sub.2 are as described above with the compound of the formula ##STR3## wherein Ar is as described above, in an aromatic organic compound. The intermediates formed by the process of the invention are useful in the production of thiazepin-4(5H)-ones which have activity as calcium channel blockers and accordingly are useful as agents for lowering blood pressure and agents for treating ischemia.

摘要翻译： 制备式IV化合物的方法，其中R 1和R 2各自独立地为氢，1至4个碳原子的烷基，1至4个碳原子的烷氧基，卤素，三氟甲基或硝基; 或者R 1和R 2与它们所连接的苯环一起为萘，Ar为对低级烷氧基苯基。 其中包括使其中R 1和R 2如上所述的其中Ar如上所述的式IIIa化合物在芳族有机化合物中反应。 通过本发明的方法形成的中间体可用于制备具有钙通道阻断剂活性的硫氮平-4（5H）酮，因此可用作降低血压的药剂和用于治疗缺血的药剂。

公开(公告)号：US4739049A

公开(公告)日：1988-04-19

申请号：US897456

申请日：1986-08-15

申请人： Robert Y. Ning ,  Pradeep B. Madan

发明人： Robert Y. Ning ,  Pradeep B. Madan

IPC分类号： C07D215/22 ,  C07D215/227 ,  C07D215/38 ,  C07D243/14 ,  C07D243/16 ,  C07D243/20 ,  C07D243/22 ,  C07D243/24 ,  C07D487/04 ,  C07D491/04 ,  C07F9/645

CPC分类号： C07D215/227 ,  C07D215/38 ,  C07D243/14 ,  C07D243/16 ,  C07D243/20 ,  C07D243/22 ,  C07D243/24 ,  C07D487/04 ,  C07D491/04 ,  C07F9/645

摘要： Compounds of the general formula ##STR1## are reacted with a strong base followed by a phosphorylating agent, such as dicyclicaminophosphinic halide or bis-di-lower alkylaminophosphinic halide to produce an imine of the formula ##STR2## wherein R is dicyclicaminophosphinyloxy or bis-di-lower alkylaminophosphinyloxy.R represents a leaving group which will undergo nucleophilic displacement with nitrogen, oxygen, sulfur and carbon containing nucleophiles, that is, nucleophiles which have, as a reactive site, a nitrogen, oxygen, sulfur or carbon atom, such that, when the cyclic imine undergoes nucleophilic displacement, there is formed C--N, C--O, C--S and C--C bonds between the carbon atom of the cyclic imine and the nucleophilic group.The end products may be utilized as intermediates in the production of pharmaceutically valuable compounds and, in some instances, are pharmaceutically valuable compounds per se.

摘要翻译： 使通式为“IMAGE”的化合物与强碱接触，然后与磷酸化试剂例如二环氨基二膦酰卤或双 - 二 - 低级烷基氨基膦化合物反应生成下式的亚胺：其中R是二环丙氨基磷酰氧基或二 - 二 低级烷基氨基磷酰氧基。 R表示将经受氮，氧，硫和碳的亲核试剂进行亲核取代的离去基团，即具有作为反应位点的氮，氧，硫或碳原子的亲核试剂，使得当环状亚胺 经过亲核取代，在环状亚胺的碳原子和亲核基团之间形成CN，CO，CS和CC键。 最终产物可以用作生产药用有价值化合物的中间体，并且在某些情况下可以是药学上有价值的化合物本身。