156715-06-9Relevant academic research and scientific papers
Chiral 1,3,2-Diazaphospholenes as Catalytic Molecular Hydrides for Enantioselective Conjugate Reductions
Miaskiewicz, Solène,Reed, John H.,Donets, Pavel A.,Oliveira, Caio C.,Cramer, Nicolai
supporting information, p. 4039 - 4042 (2018/03/13)
Secondary 1,3,2-diazaphospholenes have a polarized P?H bond and are emerging as molecular hydrides. Herein, a class of chiral, conformationally restricted methoxy-1,3,2-diazaphospholene catalysts is reported. We demonstrate their catalytic potential in asymmetric 1,4-reductions of α,β-unsaturated carbonyl derivatives, including enones, acyl pyrroles, and amides, which proceeded in enantioselectivities of up to 95.5:4.5 e.r.
Development of biisoquinoline-based chiral diaminocarbene ligands: Enantioselective SN2′ allylic alkylation catalyzed by copper-carbene complexes
Seo, Hwimin,Hirsch-Weil, Dimitri,Abboud, Khalil A.,Hong, Sukwon
, p. 1983 - 1986 (2008/09/19)
Chiral biisoquinoline-based diaminocarbene ligands (BIQ) were designed to create a chiral environment extended toward the metal center, which was confirmed by an X-ray structure. The concise ligand synthesis is highlighted by a modified Bischler-Napieralski cyclization of bisamides prepared from readily available chiral phenethylamines, and allows easy variation of the stereodifferentiating groups. The cyclohexyl-BIQ-copper complex is an efficient catalyst for enantioselective SN2′ allylic alkylation with Grignard reagents showing SN2′ regioselectivity higher than 5:1 and enantioselectivity in the range of 68-77% ee.
Irreversible HIV protease inhibitors, compositions containing same and process for the preparation thereof
-
, (2008/06/13)
The present invention relates to novel compounds of formula (I) which has inhibitory activities against human immunodeficiency virus ("HIV") protease, a process for the preparation thereof, and compositions for prevention or treatment of AIDS by HIV infec
Irreversible HIV protease inhibitors, compositions containing same and process for the preparation thereof
-
, (2008/06/13)
The present invention relates to novel compounds of formula (I) which has inhibitory activities against human immunodeficiency virus ("HIV") protease, a process for the preparation thereof, and compositions for prevention or treatment of AIDS by HIV infection comprising the above compounds as active ingredients. wherein: R1is an aromatic group, a nitrogen-containing aromatic group, C1-4alkyl group optionally substituted with an aromatic group or a nitrogen-containing aromatic group, C1-4alkoxy group optionally substituted with an aromatic group or a nitrogen-containing aromatic group; R2is an amino acid residue or a C1-8alkyl group substituted with a C1-4alkylsulfonyl group; R3is a C1-4alkyl group optionally substituted with an aromatic group; R4is hydrogen or a C1-2alkyl group; R5is a C1-10alkyl group optionally substituted with an aromatic group; and n is 1 or 2.
An efficient and enantioselective synthesis of a chiral primary amine
Son, Youngchan,Park, Chihyo,Koh, Jong Sung,Choy, Nakyen,Lee, Chang S.,Choi, Ho-Il,Kim, Sung Chun,Yoon, Heungsik
, p. 3745 - 3746 (2007/10/02)
An efficient and enantioselective method for the preparation of a chiral primary amine has been developed. Starting from N-protected L or D-amino acid the sequence involves coupling with N-methoxy-N-methylamine, acylation, olefination with potassium bis(trimethylsilyl)amide, and hydrogenation.
N-(Trifluoroacetyl)-α-amino Acid Chlorides as Chiral Reagents for Friedel-Crafts Synthesis
Nordlander, J. Eric,Njoroge, F. George,Payne, Mark J.,Warman, Dhiraj
, p. 3481 - 3484 (2007/10/02)
Chiral N-(trifluoroacetyl)-α-amino acid chlorides unergo Friedel-Crafts reaction with benzene and 1,2-dimethoxybenzene under mild conditions commonly with complete (>99percent) preservation of configurational identity.The resultant (trifluoroacetyl)amino ketones may be deoxygenated with Et3SiH or H2/Pd-C in acidic media to the corresponding N-(trifluoroacetyl)-β-arylalkylamines likewise without loss of configurational purity.
