专利号:US-6340751-B1 优先权日:1998-07-24 标 题 :Process for the preparation of 4-substituted azetidinone derivatives 发明人:SAITO TAKAO; MURAYAMA TOSHIYUKI; MATSUMOTO TAKAJI; MIURA TAKASHI 权利人:TAKASAGO PERFUMERY CO LTD 摘要:Disclosed is a process for the preparation of a 4-substituted azetidinone derivative, which comprises reacting an azetidinone derivative and an amide compound in the presence of a magnesium compound such as those represented by the following formulas (II): n and (IV): n represented by the following formula (III): n n n MgR 5 R 6   (III) n n n wherein R 5 represents a C 1-12 alkyl group, a C 2-5 alkenyl group, a 5- to 8-membered alicyclic group which may be substituted by a lower C 1-4 alkyl group, a phenyl group which may be substituted by a lower C 1-4 alkyl group, a lower C 1-4 alkoxy group or a halogen atom or a benzyl group which may be substituted by a lower C 1-4 alkyl group, a lower C 1-4 alkoxy group or a halogen atom, and R 6 represents a halogen atom, a methanesulfonyloxy group, a benzenesulfonyloxy group, a p-toluenesulfonyloxy group, a trifluoromethanesulfonyloxy group, an acetoxy group which may be substituted by a halogen atom or a cyano group or an OR 7 group (R 7 representing a lower C 1-4 alkyl group, a substituted or unsubstituted phenyl group or a substituted or unsubstituted benzyl group). The process provides an industrially excellent process for the preparation of a 4-substituted azetidinone derivative which permits the selective preparation of an intermediate for the synthesis of a carbapenem antibacterial agent having a desired 1-β′ configuration.
专利号:US-4246176-A 优先权日:1979-07-05 标 题 :Synthesis of 5-aroyl-1-hydrocarbylpyrrole-2-acetic acid 发明人:ZAIKO EDWARD J 权利人:ETHYL CORP 摘要:The reaction between a 5-cyano-1-hydrocarbylpyrrole-2-acetic acid and an aryl Grignard compound to produce a ketimine salt-containing reaction intermediate is improved by performing such reaction in an aromatic ether reaction medium at a temperature above about 100° C. As compared to the previously known process, the reaction rate is markedly increased without loss of selectivity. Also, the water insolubility of aromatic ethers simplifies product work-up and recovery, reduces product losses, and facilitates solvent recovery and recycle. Preferably, the aryl Grignard reagent is prepared at the outset in tetrahydrofuran or methyl tetrahydrofuran--solvents in which such Grignard reagents are readily and safely produced. The resultant Grignard solution may then be employed in forming the aromatic ether-containing reaction medium in which the above reaction is conducted.
专利号:US-8207337-B2 优先权日:2007-01-29 标 题:Reagent for organic synthesis reaction containing organic triol borate salt 发明人:MIYAURA NORIO; YAMAMOTO YASUNORI 权利人:MIYAURA NORIO; YAMAMOTO YASUNORI; WAKO PURE CHEM IND LTD 摘要:[Problem] n To provide an organoboron compound-containing reagent for organic synthesis reactions which undergoes no trimerization with dehydration, does not necessitate activation with a base, and is stable and highly active. n [Means for Solving Problems] n The reagent for organic synthesis reactions contains an organic triol borate salt represented by any of the general formulae (I) to (III) and general formula (XVI): (wherein R 1 represents alkyl, alkenyl, etc.; R 2 represents optionally substituted alkyl, alkenyl, alkynyl, etc. or represents hydrogen; m + represents an alkaline metal ion, phosphonium ion, or given ammonium ion; M 2+ represents an alkaline earth metal; X represents halogen or alkoxide; Y represents an alkali metal ion, etc.; A represents optionally substituted methylene; and n represents an integer).
专利号:WO-2011000532-A2 优先权日:2009-07-03 标题:Method for the enantioselective addition of organometallic carbon nucleophiles to trifluoromethyl ketones and use of the method in the synthesis of hiv reverse transcriptase inhibitors
专利号:US-4474703-A 优先权日:1976-11-09 标 题 :Grignard reagents and processes for making and using them 发明人:BUJADOUX KAREL; NEYER JEAN-MARIE; HOUZEAUX JEAN-PIERRE 权利人:CHARBONNAGES STE CHIMIQUE 摘要:An organometallic halide having the formula: (RMX) (MX2)a(MR2)b (MH2)c wherein a=0.45, b=0.15, and c=0.30, X is a halogen, R is a hydrocarbon radical, and M is a metal selected from the group consisting of magnesium, zinc, beryllium, and calcium is prepared by a continuous dry process by reacting an organic monohalide RX and a metal M in the form of convex solid grains of a size between 1 and 15 mm. The reaction temperature is lower than the temperature at which decomposition of the organometallic halide RMX begins and at least 10 DEG C. higher than the boiling point of the organic monohalide. The reaction may also take place in the presence of an organometallic derivative comprising a hydroxy group or an enolysable ketone group. The resulting organometallic halide may be used for the synthesis of anhydrous magnesium halide or for the reduction of titanium tetrachloride.
专利号:US-6417400-B1 优先权日:1998-03-24 标题:Methyl-phenyl derivatives, preparation method and use 发明人:DORMOY JEAN-ROBERT; GOUBET DOMINIQUE; MOREAU PATRICE 权利人:SANOFI SYNTHELABO 摘要:The present invention relates to:a) methylbiphenyl derivatives of general formula:in which R1 represents OH, C3-C7 alkyl or C3-C7 cycloalkyl, these compounds being in the form of individual isomers or mixtures thereof,b) their preparation by reaction:either of a hydroxylamine salt with an N-substituted o-(p-tolyl)benzaldimine, to give o-(p-tolyl)benzaldoximeor of an N-substituted 2-halobenzaldimine with a p-tolylmagnesium halide in the presence of an inorganic manganese derivative, to give the compounds of formula I in which R1 represents C3-C7 alkyl or C3-C7 cycloalkylc) their use for the preparation of o-(p-tolyl)-benzonitrile, which is an intermediate in the synthesis of medicinal products.