46114-16-3Relevant articles and documents
Rapid, one-pot synthesis of α,α-disubstituted primary amines by the addition of Grignard reagents to nitriles under microwave heating conditions
Gregg, Brian T.,Golden, Kathryn C.,Quinn, John F.,Wang, Hong-Jun,Zhang, Wei,Wang, Ruifang,Wekesa, Francis,Tymoshenko, Dmytro O.
experimental part, p. 3978 - 3981 (2009/10/04)
A series of α,α-disubstituted amines have been prepared in a simple and efficient one-pot procedure by the addition of Grignard reagents to a series of aliphatic, aromatic, and heteroaromatic nitriles. Key to this reported procedure is the unprecedented addition of the Grignard reagent to the nitrile under heating by microwave irradiation which both significantly improves reaction yields and reduces reaction times. In general, the Grignard addition reaction is complete within 5-10 min at 100 °C followed by rapid reduction with sodium borohydride to give the target amines.
Convenient Access to Primary Amines by Employing the Barbier-Type Reaction of N-(Trimethylsilyl)imines Derived from Aromatic and Aliphatic Aldehydes
Gyenes, Ferenc,Bergmann, Kathryn E.,Welch, John T.
, p. 2824 - 2828 (2007/10/03)
A new versatile preparation of primary amines via benzylation of aromatic and aliphatic aldimines is described. Sonochemical and traditional methods for generation of the reactive intermediates are compared and contrasted. Competitive reactions were analyzed via free energy relationships to support the proposed alkylative mechanism.
Irreversible HIV protease inhibitors, compositions containing same and process for the preparation thereof
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, (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.