- A preparation containing [...] method for synthesizing of antihypertensive medicines we surround class
-
The invention relates to a synthesis method for preparing an antihypertensive medicine having a benzofuroxan ring. In the method, 4-methylbenzofuroxan is used as a raw material, the 2,1,3-benzoxadiazole-4-aldehyde serving as an important intermediate is prepared by bromination and oxidation reactions, and the 2,1,3-benzoxadiazole-4-aldehyde and acetoacetic ester undergo a Hantzsch reaction to form the target compound. Compared with other processes, the method has the characteristics of mild reaction conditions, simple and efficient operation, high yield and the like and has a certain industrial production prospect.
- -
-
-
- The accelerated preparation of 1,4-dihydropyridines using microflow reactors
-
The synthesis of 1,4-dihydropyridines was performed in a continuous-flow microreactor. Elevated temperatures accelerated the reaction rate significantly allowing the reaction to be finished in minutes (6-11 min). Different 1,4-dihydropyridines were prepared in good to excellent isolated yields (45-88% yield). The method was amenable to the preparation of daropidine, a calcium channel blocker which is currently in clinical phase 3 trials.
- Baraldi, Patricia Tambarussi,No?l, Timothy,Wang, Qi,Hessel, Volker
-
supporting information
p. 2090 - 2092
(2014/04/03)
-