1159735-22-4Relevant articles and documents
Development of a Scalable Route for a Highly Polar Heterocyclic Aminocyclopropyl Building Block
Abele, Stefan,Ahmetovic, Muhamed,Fleischer, Tony,Sch?fer, Gabriel
, p. 1735 - 1742 (2020)
A robust and scalable route toward key heterocyclic building block 1-(pyrimidin-2-yl)cyclopropan-1-amine hydrochloride from cyclopropanated starting material 1-amino-1-cyclopropanecarbonitrile hydrochloride was successfully developed. The key to success was the construction of a pyrimidine ring via cyclization from an amidine intermediate and a bench-stable 2-chloro vinamidinium hexafluorophosphate salt. The cyclization was performed under mild conditions, and the resulting 4-cloropyrimidine derivative was isolated in high yield and purity. The final hydrogenation was intensively optimized: A combination of Pd(OH)2/C as a catalyst and NaOMe as a base at 1 bar H2 pressure in MeOH simultaneously cleaved the Cbz group and dechlorinated the pyrimidine ring while at the same time suppressing the over-reduction of the pyrimidine ring to below 1.0%. After acidification with HCl, followed by removal of the catalyst and NaCl by filtration, the final product was isolated in high yield and purity as a bench-stable off-white solid. The overall yield of the five-step sequence was 57%.
CARBONYL DERIVATIVES OF BETULIN
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, (2013/03/26)
Disclosed are a compound characterized by the following formula I or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising said compound or a pharmaceutically acceptable salt thereof, wherein R3, L, and A are as described in the application. Said compounds are useful for the treatment of HIV.
DERIVATIVES OF 6,7-DIHYDRO-5H-IMIDAZO[1,2-α]IMIDAZOLE-3- CARBOXYLIC ACID AMIDES
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Page/Page column 156, (2009/07/03)
Derivatives of 6,7-dihydro-5H-imidazo[1,2-α]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
