4430-75-5Relevant articles and documents
Biocatalytic Access to Piperazines from Diamines and Dicarbonyls
Borlinghaus, Niels,Gergel, Sebastian,Nestl, Bettina M.
, p. 3727 - 3732 (2018/04/14)
Given the widespread importance of piperazines as building blocks for the production of pharmaceuticals, an efficient and selective synthesis is highly desirable. Here we show the direct synthesis of piperazines from 1,2-dicarbonyl and 1,2-diamine substrates using the R-selective imine reductase from Myxococcus stipitatus as biocatalyst. Various N- and C-substituted piperazines with high activity and excellent enantioselectivity were obtained under mild reaction conditions reaching up to 8.1 g per liter.
6' SUBSTITUTED COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY
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Page/Page column 39; 40, (2008/12/08)
The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): wherein R1—R4 A, B, D, E, and G are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
BICYCLIC NONANE AND DECANE COMPOUNDS HAVING DOPAMINE RECEPTOR AFFINITY
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, (2008/06/13)
Described herein are D4 receptor-selective compounds of the general formula: STR1 wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5-or 6-membered, homo-or heterocyclic rings;X 1 is selected from CH 2, O, NH, S, C=O, CH--OH, CH--N(C 1-4 alkyl) 2, C=CHCl, C= CHCN, N-C 1-4 alkyl, N-acetyl, SO 2 and SO;X. sub.2---is selected from N=, CH 2--, CH=, C(O)--, O--, and S--;n is 1 or 2;R 1 is selected from H and an amino acid side chain;R 2 is selected from H, OH, C 1-9 alkyl, C 1-9 alkoxy, and benzyloxy; andR 3 is selected from H, OH, halo, cyano, C 1-4 alkyl, C 1-4 alkoxy, phenoxy, benzyloxy, =O, =S, C 1-4 alkylsulfonyl, C 1-4 alkylsulfonyl, C 1-4 alkylthio, amino, and aminocarbonyl;and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia, is also described.