179533-67-6Relevant academic research and scientific papers
PROCESS FOR PREPARATION OF BRIVARACETAM
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Paragraph 0196, (2019/05/22)
The present invention relates to a process for the preparation of brivaracetam and salts thereof. The present invention provides process for the preparation of brivaracetam and salts thereof with high chiral purity. The present invention provides process for the preparation of brivaracetam and salts thereof wherein the amount of other stereoisomers of brivaracetam is low.
TRICYCLIC HETEROCYCLIC COMPOUNDS AS NOTCH INHIBITORS
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Paragraph 00199; 00200, (2014/04/04)
Disclosed are compounds of Formula (I), wherein: X is O or -NR3; R1 is -CH2CH2CH3, -CH2CF3, -CH2CH2CF3, -CH2CF2CH3, -CH2CH2CH2CF3, -CH2CH2CF2CH3, -CH2CH(CH3)CF3, -CH2CH2CH2F, or CH2(cyclopropyl); R2 is -CH2CH2CH3, -CH2CF3, -CH2CH2CF3, -CH2CF2CH3, -CH2CH2CH2CF3, -CH2CH2CH2F, -CH2CH(CH3)CF3, CH2CH2CF2CH3, -CH2(cyclopropyl), -CH(CH3)(cyclopropyl), phenyl, fluorophenyl, chlorophenyl, trifluorophenyl, methylisoxazolyl, pyridinyl, formula (i), formula (ii), formula (iii), formula (iv) or formula (v); Ring A is phenyl or pyridinyl; and R3, Ra, Rb, Rc, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.
Syntheses of aminoalcohol-derived macrocycles leading to a small-molecule binder to and inhibitor of Sonic Hedgehog
Peng, Lee F.,Stanton, Benjamin Z.,Maloof, Nicole,Wang, Xiang,Schreiber, Stuart L.
supporting information; experimental part, p. 6319 - 6325 (2010/05/02)
We report the synthesis and biological activity of a library of aminoalcohol-derived macrocycles from which robotnikinin (17), a binder to and inhibitor of Sonic Hedgehog, was derived. Using an asymmetric alkylation to set a key stereocenter and an RCM re
Discovery of N-hydroxy-2-(2-oxo-3-pyrrolidinyl)acetamides as potent and selective inhibitors of tumor necrosis factor-α converting enzyme (TACE)
Duan, James J.-W.,Lu, Zhonghui,Xue, Chu-Biao,He, Xiaohua,Seng, Jennifer L.,Roderick, John J.,Wasserman, Zelda R.,Liu, Rui-Qin,Covington, Maryanne B.,Magolda, Ronald L.,Newton, Robert C.,Trzaskos, James M.,Decicco, Carl P.
, p. 2035 - 2040 (2007/10/03)
New inhibitors of tumor necrosis factor-α converting enzyme (TACE) were discovered using an N-hydroxy-2-(2-oxo-3-pyrrolidinyl)acetamide scaffold. The series was found to be potent in a porcine TACE (pTACE) assay with IC50s typically below 5 nM.
Synthesis of substituted cyclohexenyl-based β-amino acids by ring-closing metathesis
Abell, Andrew D.,Gardiner, James
, p. 3663 - 3666 (2007/10/03)
(equation presented) A versatile ring-closing metathesis (RCM) approach has been developed for the preparation of cis and trans cyclohexenyl-based β-amino acids that are either unsubstituted (3) or substituted (10 and 12) at the α-position.
Enantioselective syntheses of orthogonally protected tricarballylic acid esters
Harmat, Nicholas J. S.,Mangani, Silvia,Perrotta, Enzo,Giannotti, Danilo,Nannicini, Rossano,Altamura, Maria
, p. 1261 - 1264 (2007/10/03)
3(S) and 3(R)-Benzyloxycarbonyl-pentanedioic acid mono-tert-butyl esters (6) were obtained as enantiopure orthogonally protected tricarballylic acid (TCA) esters. These were synthesised by alkylation of the sodium enolate derived from chiral but-3-enoylox
