116199-87-2

A general route to a series of novel imidazobenzazepines that are 'carba' analogs of the TIBO class of non-nucleoside HIV-1 reverse transcriptase inhibitors has been developed. A pair of allyl side-chain containing compounds were found to have significant HIV-1 inhibitory activity.

The invention relates to a method for preparing 2, 3-dihydro-2-oxo-1H-benzimidazole-1-butyric acid, which comprises the following steps of: dehydrating 1, 3-dihydro-1-(1-methylvinyl)-2H-benzimidazole-2-one in an organic solvent at 100-120 DEG C under the action of an acid-binding agent, adding ethyl 4-bromobutyrate for reaction after dehydration, cooling the reaction liquid to 70-90 DEG C after the reaction is finished, adding water preheated to 40-60 DEG C, stirring and splitting phases at proper time; and adding alkali into an organic phase, carrying out saponification reaction under the environment of 45-80 DEG C and 150-200 mbar, slowly adding hydrochloric acid at the temperature of 40-60 DEG C after the saponification reaction is finished, then reacting for 2-4 hours at the temperature of 90-110 DEG C, cooling, filtering, washing a filter cake with water, and drying the filter cake to constant weight at 50-70 DEG C and 100-180 mbar. Potassium carbonate is used to replace sodium hydride, so that the problems of high potential safety hazard, serious three-waste pollution and the like in the traditional process are fundamentally eliminated, the production process is simpler and more convenient by frying in one pot, and the production cost is reduced; and meanwhile, the method is simple, convenient and safe to operate, reasonable in process condition, high in reaction yield and relatively high in implementation value.

Compounds of formula (I) and pharmaceutically acceptable salts thereof are agonists at the beta-2 adrenoceptor. They are useful as feed additives for livestock animals.

Compounds of formula (I) and pharmaceutically acceptable salts thereof are agonists at the beta-2 adrenoceptor. They are useful as feed additives for livestock animals.

Novel 6-amino-7-hydroxy-4,5,6,7-tetrahydro-imidazo[4,5,l-j-k][1]-benzazepin-2-(1H)-one derivatives of the formula STR1 wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms optionally substituted with a hydroxyl, aryl and aryloxy of 6 to 10 carbon atoms, cycloalkyl of 3 to 7 carbon atoms optionally interrupted with a heteroatom optionally substituted with alkyl of 1 to 4 carbon atoms and the wavy lines indicates that the 7-OH and 6-amino have the trans configuration and their non-toxic, pharmaceutically acceptable acid addition salts having remarkable anti-hypertensive and hypotensive activity and vasodilatatory activity and their preparation.