2144-87-8Relevant articles and documents
Purine derivative and preparation method and application thereof
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Paragraph 0181; 0419-0420, (2021/06/26)
The invention discloses a purine derivative and a preparation method and application thereof, belongs to the technical field of medicines, and designs and synthesizes a series of purine derivatives and optical isomers, pharmaceutically acceptable salts, solvates or prodrugs of the purine derivatives. Experiments show that the compound has outstanding anti-cell proliferation activity and DOT1L enzyme inhibition effect, shows good tumor growth inhibition activity in a tumor transplantation tumor model, and has a good application prospect.
Octahydrocyclopenta[c]pyrrole Allosteric Inhibitors of SHP2
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Paragraph 0446-0449, (2019/03/30)
The present invention relates to compounds capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds, and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.
An Efficient and Scalable Synthesis of tert-Butyl (3aR,6aS)-5-Oxohexahydrocyclo penta[c]pyrrole-2(1H)-carboxylate: A Pharmacologically Important Intermediate
Bahekar, Rajesh H.,Jadav, Pradip A.,Goswami, Amitgiri D.,Shah, Hardik A.,Dave, Bhushan N.,Joshi, Darshan A.,Pethani, Jignesh P.,Patel, Dipam,Agarwal, Sameer,Desai, Ranjit C.
, p. 266 - 272 (2017/02/26)
Hexahydrocyclopentapyrrolone derivatives constitute an important class of bicycles, and it represents an essential pharmacophore for diversified pharmacological activities. A highly efficient process for the synthesis of tert-butyl(3aR,6aS)-5-oxohexahydrocyclopenta[c]pyrrole-2(1H)-carboxylate 1 has been developed. The improved process involves transformation of isoindole 4 to diacid 5, using an inexpensive KMnO4 mediated oxidative cleavage as a key step. The developed process was cost-effective, high yielding, kilogram scalable, and commercially viable for synthesis of 1.