专利号:US-5519128-A 优先权日:1993-03-31 标题:Process for the synthesis of acylated derivatives of fatty acid-transporting thiols and in particular acyl-coenzymes A and the thus obtained acyl-coenzymes A 发明人:LELLOUCHE JEAN-PAUL; LEVANNIER KARINE; MIOSKOWSKI CHARLES 权利人:COMMISSARIAT ENERGIE ATOMIQUE 摘要:The invention relates to a process for the synthesis of an acylated derivative of a fatty acid-transporting thiol such as the coenzyme A. According to this process, a silylated or stannylated thiol is prepared by reacting the thiol with a silylation or stannylation reagent in order to at least partly replace the unstable hydrogens of the thiol by SiR3 or SnR3 groups with R being an alkyl or aryl group. The silylated or stannylated thiol is then reacted in an anhydrous organic medium with an activated organic acid and a deprotection reagent able to eliminate the silyl or stannyl groups. In this way it is possible to obtain acylated derivatives of the coenzyme A, in which the acyl group can have up to 30 carbon atoms with high yields.
专利号:US-6924375-B2 优先权日:2003-09-03 标题:Facile synthesis of 1,9-diacyldipyrromethanes 发明人:LINDSEY JONATHAN S; TAMARU SHUN-ICHI; YU LIANHE 权利人:UNIV NORTH CAROLINA STATE 摘要:The present invention provides a method of making a metal complex. The method comprises the steps of: (a) acylating a dipyrromethane or a 1-monoacyldipyrromethane to form a mixed reaction product comprising a 1,9-diacyidipyrromethane; (b) combining the reaction product with a compound of the formula R 2 MX 2 in the presence of a base, where R is alkyl or aryl, M is Sn, Si, Ge, or Pb (preferably Sn), and X is halo, OAc, acac, or OTf, to form a product comprising a metal complex of the formula DMR 2 in the mixed reaction product, wherein D is a 1,9-diacyldipyrromethane; and then (c) separating the metal complex from the mixed reaction product. The method may be utilized for the convenient synthesis and separation of 1,9-diacyldipyrromethanes. Metal complex intermediates useful in such methods are also described.
专利号:US-9265773-B2 优先权日:2011-09-08 标题 :Tetracyclic heterocycle compounds and methods of use thereof for the treatment of viral diseases 发明人:MCCOMAS CASEY C; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO; PALANI ANANDAN; HE SHUWEN; DAI XING; LIU HONG; LAI ZHONG; LONDON CLARE; XIAO DONG; ZORN NICOLAS; NARGUND RAVI 权利人:MCCOMAS CASEY C; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO; PALANI ANANDAN; HE SHUWEN; DAI XING; LIU HONG; LAI ZHONG; LONDON CLARE; XIAO DONG; ZORN NICOLAS; NARGUND RAVI; MERCK SHARP & DOHME; MSD ITALIA SRL 摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
专利号:US-7517828-B2 优先权日:2003-04-25 标 题 :Chiral broensted acid catalyst for asymmetric synthesis and method of asymmetric synthesis with the catalyst 发明人:AKIYAMA TAKAHIKO 权利人:TOAGOSEI CO LTD 摘要:A compound usable as an asymmetric synthesis catalyst which can be easily synthesized without using any metal such as a lanthanoid group element; a method of asymmetric synthesis with the compound; and a chiral compound obtained by the asymmetric synthesis method. A Broensted acid is used as a catalyst in asymmetric synthesis, the chiral Broensted acid being represented by formula (1) below or formula (3) below. The asymmetric synthesis method employs the catalyst. Asymmetric synthesis with the catalyst gives a chiral compound.
专利号:US-6271391-B1 优先权日:1998-03-13 标题 :Hydrazide fixed to a resin and derivatives thereof, and a method for synthesizing pyrazolones in solid phase 发明人:KOBAYASHI SHU; OYAMADA HIDEKAZU 权利人:JAPAN SCIENCE & TECH CORP 摘要:Hydrazide fixed to a resin represented by the following formula: n n n P—Q—CO—NH—NH 2   (I) n n n where P represents a main chain of a resin polymer and Q represents a hydrocarbon side chain optionally having a substituent which may be bonded via a heteroatom, and a hydrazone derived therefrom and fixed to a resin n n n P—Q—CO—NH—Nâ•?CH—R 1   (II) n n n are provided, and solid phase synthesis of pyrazolone is conducted using the same, thereby enabling synthesis of pyrazolones by the application of the Mannich type reaction based on the solid phase synthesis and efficient construction of libraries for various kinds of them.
专利号:US-6417368-B1 优先权日:1998-03-13 标题:Amine derivative fixed to resin and method for synthesizing β-aminocarbonyl compound in a solid phase 发明人:KOBAYASHI SHU; AOKI YOJI 权利人:JAPAN SCIENCE & TECH CORP 摘要:The invention provides a resin-immobilized imine represented by the following formula: n n n P—Q—N—â•?CH—R   I n n n [in the formula, P represents the principal chain of a resin polymer; Q represents a substituted or unsubstituted hydrocarbon side chain or a substituted or unsubstituted hydrocarbon side chain with a heteroatom interposed therein; R represents a substituted or unsubstituted hydrocarbon group or heterocyclic group] and a resin-immobilized β-aminocarbonyl compound of the following formula: n which can be released as β-aminocarbonyl compound from the solid phase; and the invention also provide a resin-immobilized amine of the following formula: n n n —P—Q 1 —O—Q 2 —NH 2   III n n n [Q 1 and Q 2 independently represent a hydrocarbon chain such as arylene, alkylenearylene or arylenealkylene], which is essential for solid state synthesis; and the invention has enabled the solid state synthesis of ²-aminocarbonyl compound by the application of iminoaldol reaction.