A process for the preparation of 1,2,3,4,8,9,10,10a-octahydro-7bH-cyclopenta[b][1,4]diazepino[6,7,1-hi]indole |
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| Authors: | Gregory S Welmaker Joan E Sabalski |
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| Institution: | a Wyeth Research, Chemical and Screening Sciences, 500 Arcola Road, Collegeville, PA 19426 USA
b Wyeth Research, Chemical and Screening Sciences, CN 8000, Princeton, NJ 08543 USA |
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| Abstract: | A synthesis of 1,2,3,4,8,9,10,10a-octahydro-7bH-cyclopentab]1,4]diazepino6,7,1-hi]indole is described exemplifying a new synthetic route to medicinally interesting compounds. The key step involves a cyclization of 2-(2,3,3a,8b-tetrahydrocyclopentab]indol-4(1H)-yl)-ethanamine with aqueous formaldehyde in the presence of trifluoroacetic acid. |
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| Keywords: | Benzodiazepine Pictet-Spengler |
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