Process Development of 5-Fluoro-3-[3-[4-(5-methoxy-4-pyrimidinyl)-1- piperazinyl]propyl]-1H-indole Dihydrochloride
✍ Scribed by Anderson, Neal G.; Ary, Thomas D.; Berg, James L.; Bernot, Peter J.; Chan, Yeung Y.; Chen, Chien-Kuang; Davies, Merrill L.; DiMarco, John D.; Dennis, Ronald D.; Deshpande, Rajan P.
- Book ID
- 115448461
- Publisher
- American Chemical Society
- Year
- 1997
- Tongue
- English
- Weight
- 334 KB
- Volume
- 1
- Category
- Article
- ISSN
- 1083-6160
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## Abstract The synthesis of 5‐Fluoro‐3‐[3‐[4‐(2‐[^14^C]‐5‐methoxy‐4‐pyrimi‐dinyl)‐1‐piperazinyl]propyl]‐1H‐indole dihydrochloride (5) was achieved by coupling [^14^C] formamidine acetate (1) and dimethylmethoxymalonate in methanol containing sodium methoxide at 60°C to provide 2‐[^14^C] 4,6‐dihydr
## Abstract The title compound was prepared by the LiAlT~4~ reduction of 5‐fluoro‐3‐[3‐[4‐(5‐methoxy‐4‐pyrimidinyl)‐1‐piperazinyl]‐3‐oxopropyl]‐1H‐indole. The radiochemical purity of the product was 98.9% and the specific activity was calculated as 53.0 Ci/mmol from HPLC analyses and 55.6 Ci/mmol f
The crystal structure of the title compound, C 21 H 18 N 2 O 5 , was determined in order to study the electrocyclic reactivity of 3,4diaryl-1H-pyrrole-2,5-dione derivatives. Intermolecular hydrogen bonds form sheets.