2-异丙基-1,3-二氢-4(1H)异喹啉酮及其衍生物的合成

Synthesis of 2-Isopropyl-1,3-Dihydro-4(1H) Isoquinolone and Its Derivatives

异喹啉酮类化合物具有重要药理活性,本文在合成1,2,3,4-四氢-2-苄基异喹啉酮-4衍生物的基础上,参照Hinton方法制备2-异丙基-1,3-二氢-4（1H）异喹啉酮（1）,用（1）进一步与芳醛、羟胺、酰氯及苯肼反应得到了相应的衍生物（3a—6e）;由（1）同NaN3反应得到了苯并二氮杂酮（7）,由（2）和肼类还合成了异喹啉并吡唑化合物(8a-d),整个反应式如下:

Compound (2) was synthesized through condensation of ethyl N-isoproyl-N-(2-car-boethoxy benzyDglycinate. Compound (1) was obtained from the hydrolysis and decarboxylation of (2) in the presence of 18% HC1. Derivatives of (1) , (3a- 6e) were produced by condensation of (1) with benzaldehyde and p-substituted benzaldehyde , phenylhydrazines and oxime or (4) with benzoyl chlorides, respectively. Benzodiazepinone (7) was prepared by Beckmann rearrangement of (4) or reaction of (1) with NaN3. Pyrazolo-isoquinolones(8a-d) were synthesized through the condensation of (2) with hydrazine or substituted hydrazine, respectively. The structures of 20 new compounds have been confirmed by element analysis, IR and JH NMR.