93288-20-1Relevant articles and documents
PD-1/PD-L1 INHIBITORS
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Page/Page column 140-141, (2019/11/12)
Compounds and methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are disclosed Formula (I)
Zr-mediated synthesis of chiral cyclic imines and their application in Betti reactions
Speich, Elena,Banfi, Luca,Moni, Lisa,Riva, Renata,Rocca, Valeria,Basso, Andrea
, p. 329 - 333 (2018/05/28)
[Figure not available: see fulltext.] A novel synthetic strategy has been outlined to assemble enantiomerically pure Betti bases with unprecedented structures. This involves the Zr-mediated reduction of pyrrolidin-2-ones to cyclic imines and their subsequent reaction with phenolic derivatives.
AGENTS FOR TREATING PAIN AND USES THEREOF
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Paragraph 0873, (2014/06/25)
This invention relates to: (a) compounds and salts thereof that, inter alia, treat pain; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
Straightforward synthesis of non-natural l-chalcogen and l-diselenide N-Boc-protected-γ-amino acid derivatives
Kawasoko, Cristiane Y.,Foletto, Patricia,Rodrigues, Oscar E. D.,Dornelles, Luciano,Schwab, Ricardo S.,Braga, Antonio L.
, p. 5173 - 5183 (2013/08/15)
The synthesis of new chiral seleno-, telluro-, and thio-N-Boc-γ-amino acids is described herein. These new compounds were prepared through a simple and short synthetic route, from the inexpensive and commercially-available amino acid l-glutamic acid. The products, with a highly modular character, were obtained in good to excellent yields, via hydrolysis of chalcogen pyroglutamic derivatives with overall retention of the l-glutamic acid stereochemistry. Also, an l-diselenide-N-Boc-γ-amino acid was prepared in good yield. This new synthetic route represents an efficient method for preparing new l-chalcogen- and l-diselenide-γ-amino acids with biological potential.
Late-stage diversification of chiral N-heterocyclic-carbene precatalysts for enantioselective homoenolate additions
Zheng, Pinguan,Gondo, Chenaimwoyo A.,Bode, Jeffrey W.
scheme or table, p. 614 - 620 (2011/10/12)
A library of chiral triazolium salts has been prepared by late-state diversification of a triazolium amine salt. By utilizing a primary amine as a functional handle, a single triazolium salt can be transformed into a variety of chiral N-heterocyclic carbene precatalysts. This approach makes the preparation of chiral N-heterocyclic carbenes possible by a single-step modification of a triazolium salt, rather than the usual need for multistep organic synthesis and challenging heterocycle formation for each member of a catalyst library. We have screened these catalysts for control of diastereo- and enantioselectivity in a γ-lactam-forming reaction between α,β-unsaturated aldehydes and cyclic ketimines. Saving the best for last: Enantioselective homoenolate additions have been hindered by the challenge of synthesizing N-mesityl-substituted azolium salts. A library of pyrrole-functionalized chiral triazolium salts was prepared by direct modification of the preformed azolium core. Copyright
Synthesis of chiral bifunctional (Thio)urea n-heterocyclic carbenes
Brand, Jonathan P.,Siles, José Ignacio Osuna,Waser, Jér?me
supporting information; experimental part, p. 881 - 884 (2010/07/10)
The rapid and modular synthesis of the first bifunctional N-heterocyclic carbenes bearing a (thio)urea moiety as H-bond donor group was reported. Different analogues could be accessed in seven steps from cheap (S)-pyroglutamic acid in good overall yields (14-30%). The synthesized carbenes were active catalysts in the benzoin reaction. Georg Thieme Verlag Stuttgart - New York.
Nitrogen-containing bicyclic compounds active on chronic pain conditions
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Page/Page column 10, (2009/09/26)
The invention refers to compounds of general formula (I) wherein the R groups are, independently, H, C1-6alkyl, aryl, CF3; Y is CH2, C=O; X is bond, C=O, SO2, or C=N-CN; m is 0, 1; n is 0, 1; A is a heterocycle, or a phenyl group optionally substituted. The compounds are active on chronic pain conditions of different origin; they can be administered alone or with other drugs. Most of these compounds are new. The invention include a process to prepare said compounds, and pharmaceutical compositions suitable for their administration to a patient.
New chiral diamide ligands: synthesis and application in allylic alkylation
Bateman, Lorraine,Breeden, Simon W.,O'Leary, Patrick
, p. 391 - 396 (2008/09/19)
A new family of chiral diamide ligands has been designed and synthesised. These ligands have been successfully applied to an asymmetric allylic substitution reaction. A palladium complex of one of the diamide ligands achieved enantioselectivities of up to 93% in the allylic alkylation of 1,3-diphenyl-3-acetoxyprop-1-ene.
Diastereoselective synthesis of enantiopure differentially protected cis-4,5-diaminopiperidin-2-one through intramolecular transamidation
Langlois, Nicole
, p. 9531 - 9533 (2007/10/03)
The diastereoselective synthesis of enantiopure differentially protected cis-4,5-diaminopiperidin-2-one was achieved by means of conjugate addition of ammonia to an unsaturated γ-lactam and transamidation reaction with ring expansion as the main steps.
Process for preparing 5-vinyl-2-pyrrolidinone and intermediates therefor
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, (2008/06/13)
4-Amino-5-hexenoic acid is prepared by: (a) reacting 5-oxo-2-pyrrolidine-acetonitrile with hydrogen and dimethylamine in the presence of a palladium catalyst to form N,N-dimethyl-2-[5'-oxo-2'-pyrrolidine]ethylamine; (b) oxidizing N,N-dimethyl-2-[5'-oxo-2'-pyrrolidine]-ethylamine to produce the corresponding N-oxide derivative; (c) pyrolysis of the N-oxide derivative to form 5-vinyl-2-pyrrolidinone; (d) optionally, separating N,N-dimethyl-2-[5'-oxo-2'-pyrrolidine]ethylamine by-product from the 5-vinyl-2-pyrrolidinone product; and (e) hydrolyzing 5-vinyl-2-pyrrolidinone to form 4-amino-5-hexenoic acid.