CAS: 1619931-27-9; (S)-N-(3-(1-((6-(3,4-Dimethoxyphenyl)Pyrazin-2-yl)Amino)Ethyl)Phenyl)-5-Methylnicotinamide

专利信息

专利号:US-5089647-A
优先权日:1989-03-09
标题:Method for preparing intermediates for the synthesis of steroid side chains in optically active form
发明人：DELUCA HECTOR F; SCHNOES HEINRICH K; PERLMAN KATO L
权利人:WISCONSIN ALUMNI RES FOUND
摘要:This invention provides a novel method for the preparation of optically active arylalykylsulfone derivatives, having a chiral center in the alkyl moiety in either the (R)- or the (S)-configuration. These optically active sulfones find use in the stereospecific synthesis of steroid or vitamin D compounds having chiral center at either carbon 24 or carbon 25 of the side chain. The method comprises the steps of reacting an optically active sulfinate ester having a chiral center at sulfur with a racemic alkyl Grignard reagent to obtain a mixture of diastereomeric sulfoxides, separating the mixture of diastereomeric sulfoxides, and oxidizing separately each of the diastereomers to obtain the desired optically active sulfone.

专利号:EP-0468457-B1
优先权日:1990-07-24
标题 :Novel substituted piperidines and their use as inhibitors of cholesterol synthesis
发明人：MCCARTHY JAMES R; BARNEY CHARLOTTE L; WANNAMAKER MARION W
权利人:MERRELL DOW PHARMA
摘要:The present invention relates to a group of compounds which are novel substituted piperidines and which act to inhibit the synthesis of cholesterol in mammals and in fungi.

专利号:EP-2883876-A1
优先权日:2013-12-16
标 题:Stereoselective synthesis of substituted pyrrolidines
发明人：ABELE STEFAN; REBER STEFAN
权利人:ACTELION PHARMACEUTICALS LTD
摘要:The present invention relates to a halo-lactonization process for the stereoselective preparation of protected 1-(halo-methyl)-3-oxo-2-oxa-5-azabicyclo[2.2.1]heptane derivatives of formula (II)n nwherein Hal and R 1 are as defined in the description. The invention further relates to the novel compounds of formula (II), and to their further transformation to the compounds of formula (III)n nwherein R 1 , R 2 , R 3 , and R 4 are as defined in the description.

专利号:WO-2013066991-A1
优先权日:2011-10-31
标题 :Crystalline solvates of nucleoside phosphoroamidates, their stereoselective preparation, novel intermediates thereof, and their use in the treatment of viral disease
发明人：CHAMBERLAIN STANLEY; IGO DAVID; BIS JOANNA; SUKUMAR SENTHIL KUMAR KUSALAKUMARI
权利人:INHIBITEX INC
摘要:This invention is directed to novel crystalline solvates of the ( S )-P diastereomer of the anti- HCV nucleoside phosphoroamidate, (2 S )-neopentyl 2-((((2 R ,3 R ,4 R ,5 R )-5-(2-amino-6- methoxy-9H-purin-9-yl)-3,4-dihydroxy-4-methyltetrahydrofuran-2-yl)methoxy)(naphthalen- l-yloxy)phosphorylamino)propanoate (also referred to as INX-08189 or IÎ?Χ-189), and to a recrystallization method for separating the two diastereomers of INX-08189. In addition, this application relates to a novel stereoselective method for the preparation of either of the two diastereomers, and to the novel synthetic intermediates used in this stereoselective synthesis. The invention also relates to the use of the crystalline solvates to increase the liver exposure of 2'-C-methyl guanosine triphosphate from an oral dose.

专利号:US-5744595-A
优先权日:1993-12-30
标题:Propargyl modified nucleosides and nucleotides
发明人：SRIVASTAVA SURESH C; RAZA SYED KAZIM
权利人:CHEMGENES CORP
摘要:The present invention describes a novel 2'-O-alkylation reaction to produce a novel series of nucleosides carrying the 2'-O-propargyl group, using propargyl bromide, dibutyl tin oxide and tetrabutyl ammonium bromide. The procedure involves novel techniques for regioselective introduction of 2'-/3'-O-propargyl group directly on the 5'-DMT-N-protected- nucleosides using dibutyl tin oxide as a mild base in conjunction with a phase transfer catalyst, tetrabutyl ammonium bromide. The reaction process has many significant features and leads to isomeric ratios in favor of the 2'-regio isomer. This allows the synthesis of the corresponding phosphoramidites of high purity.

专利号:EP-0789577-A1
优先权日:1995-06-07
标 题:Synthesis of n-substituted oligomers