Synthesis of 1,3-dihydro-5(r)-7,8-ethylenedioxy-2h-1,4-benzo-diazepin-2-ones
β Scribed by S. S. Mochalov; D. V. Kosynkin; I. D. Yudin; V. N. Atanov; Yu. S. Shabarov; N. S. Zefirov
- Publisher
- Springer US
- Year
- 1994
- Tongue
- English
- Weight
- 486 KB
- Volume
- 30
- Category
- Article
- ISSN
- 0009-3122
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## Abstract A new method was developed for the synthesis of 6,7βdihydroβ5__H__βpyrimido[4,5β__e__][1,4]diazepinβ8(9__H__)βone derivatives. The key to construct the pyrimido[4,5β__e__][1,4]diazepine core is the intramolecular amidation of __N__β((4βaminoβ6βchloropyrimidinβ5βyl)methyl)βsubstituted am
A practical and expedient synthesis of the title compounds is described. They were prepared by Stille reaction of nitro halopyridines 4 or nitro fluro-halobenzenes 10, followed by Michael addition of tertbutyl 4-aminopiperidine-1-carboxylate to the resulting activated vinyl compounds 5 and 11, hydro