46114-16-3Relevant academic research and scientific papers
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.
Exploring the active site of phenylethanolamine N-methyltransferase: 3-alkyl-7-substituted-1,2,3,4-tetrahydroisoquinoline inhibitors
Grunewald, Gary L.,Romero, F. Anthony,Chieu, Alex D.,Fincham, Kelcie J.,Bhat, Seema R.,Criscione, Kevin R.
, p. 1261 - 1273 (2007/10/03)
A series of 3-alkyl-7-substituted-1,2,3,4-tetrahydroisoquinolines was synthesized and these compounds were evaluated for their PNMT inhibitory potency and affinity for the α2-adrenoceptor. 7-Nitro-, 7-bromo-, 7-aminosulfonyl-, or 7-N-2,2,2-trif
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 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.
Irreversible HIV protease inhibitors, intermediates, compositions and processes for the preparation thereof
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, (2008/06/13)
Novel cis-epoxide compounds of formula (I) are useful for treating or preventing diseases caused by HIV infection: STR1 wherein A, B, R1 to R4 and n have the same meanings as defined in the specification. The novel HIV protease inhib
Irreversible HIV protease inhibitors, intermediates, compositions and processes for the preparation thereof
-
, (2008/06/13)
The present invention provides cis-epoxide compounds represented by formula (I-1), (I-2) or (I-3) which are useful for treating or preventing diseases caused by HIV infection: STR1 wherein: A, B, D, E, R1, R10, R11, K, G, Q, r and J have the meanings as defined in the specification.
Irreversible HIV protease inhibitors, intermediates, compositions and processes for the preparation thereof
-
, (2008/06/13)
Novel cis-epoxide compounds of formula (I) are useful for treating or preventing diseases caused by HIV infection: wherein A, B, R1 to R4 and n have the same meanings as defined in the specification. The novel HIV protease inhibitor
Cis-epoxide derivatives useful as irreversible HIV protease inhibitors and process and intermediates for their preparation
-
, (2008/06/13)
The present invention provides cis-epoxide compounds represented by formula (I-1), (I-2) or (I-3) which are useful for treating or preventing diseases caused by HIV infection: wherein:, A, B, D, E, R1, R10, R11, K, G, Q, r and J have the meanings as defined in the specification.
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.
