867065-53-0Relevant articles and documents
Chemo-selective syntheses of: N-t -boc-protected amino ester analogs through Buchwald-Hartwig amination
Karambizi, Victoire G.,O'Brien, Gregory,Rahman, Mahmuda,Scott Goodman, M.,Suwal, Sujit,Wrotny, Matthew
supporting information, p. 2605 - 2608 (2022/02/22)
The synthesis of N-protected amino esters is achieved via a chemo-selective Buchwald Hartwig cross-coupling reaction using PEPPSI-IPr Pd-catalyst. Nearly two dozen functionally and structurally diverse amino ester molecules are created by individually cross-coupling eight aryl halo esters and three different secondary amines. We observed that product formation is more facile in those heterocyclic esters where nitrogen is present ortho to the halo substituent in the heteroaromatic ring. Based on this observation, we propose a possible intermediate step in the cross-coupling cycle, where the nitrogen electron lone pair in the heterocycle may play an important role leading to a higher reaction yield.
SELECTIVE HDAC1,2 INHIBITORS
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Paragraph 0599; 0600; 0601, (2018/06/04)
Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with HDAC1 and/or HDAC2 activity.
OXYMETHYLENE ARYL COMPOUNDS FOR TREATING INFLAMMATORY GASTROINTESTINAL DISEASES OR GASTROINTESTINAL CONDITIONS
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Paragraph 0479; 0480, (2018/03/28)
Use of oxymethylene aryl GPRl 19 agonists, and optionally DPP IV inhibitors and optionally metformin, for the treatment of inflammatory gastrointestinal diseases or gastrointestinal conditions involving malabsorption of nutrients and/or fluids are provide