CAS: 149437-76-3; 5-(4-Fluorophenyl)-5-Oxopentanoic Acid

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CAS号108-55-4 戌二酸酐 | CAS号462-06-6 氟苯 | CAS号53715-97-2 5,5'-氧双(5-氧代戊酸) | CAS号189028-93-1 (4S)-3-[5-(4-氟苯... | CAS号924909-70-6 1-(4-fluorophen...

(1S,2R)-Trans-2-(4-Fluorophenyl)-1-Cyclohexanol置于邻苯二甲酸亚胺,偶氮二甲酸二异丙酯,Rose Bengal,氧气,三苯基膦体系中,用 四氢呋喃,1,4-二氧六环 用作溶剂,化学反应 26.0H,反应生成4-(4-氟苯甲酰基)丁酸
参考文献:可见光促进伯胺的无金属有氧氧化为酸和内酯
标题:可见光促进伯胺的无金属有氧氧化为酸和内酯
摘要:通过可见光光催化双碳-碳键断裂和多碳-氢键氧化,独特地进行了伯胺的无金属好氧氧化.通过使用具有18 W Cfl的二恶烷,可以控制伯胺的好氧氧化,以提供酸;通过使用具有8 W绿色led的dmf,可以分别控制内酯的内酯.在控制实验的基础上,提出了一个合理的机制.该观察结果为脂肪族伯胺的好氧氧化中的碎片化提供了直接证据.
Doi:10.1002/chem.201604440

专利信息

专利号:US-2008032964-A1
优先权日:2006-04-10
标题:Process for the synthesis of azetidinone
发明人：KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO
权利人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO
摘要:Provided are intermediates useful for the synthesis of hydroxyl-alkyl substituted azetidinones, processes of their preparation, and processes for the synthesis of certain hydroxyl-alkyl substituted azetidinones. Also provided are processes for the synthesis of 1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone, or ezetimibe.

专利号:US-8383810-B2
优先权日:2004-12-20
标题:Process for the synthesis of azetidinones
发明人：THIRUVENGADAM TIRUVETTIPURAM K; CHIU JOHN S; FU XIAOYONG; MCALLISTER TIMOTHY L
权利人:MERCK SHARP & DOHME; THIRUVENGADAM TIRUVETTIPURAM K; CHIU JOHN S; FU XIAOYONG; MCALLISTER TIMOTHY L
摘要:A process is provided for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, comprising reacting a β-(substituted-amino)amide, a β-(substituted-amino)acid ester, or a β-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent selected from the group consisting of alkali metal carboxylates, quaternary ammonium carboxylates, quaternary ammonium hydroxides, quaternary ammonium alkoxides, quaternary ammonium aryloxides and hydrates thereof, or the reaction product of: (i) at least one quaternary ammonium halide and at least one alkali metal carboxylate; or (ii) at least one quaternary ammonium chloride, quaternary ammonium bromide, or quaternary ammonium iodide and at least one alkali metal fluoride, wherein a quaternary ammonium moiety of the cyclizing agent is unsubstituted or substituted by one to four groups independently selected from the group consisting of alkyl, arylalkyl and arylalkyl-alkyl.

专利号:US-6207822-B1
优先权日:1998-12-07
标 题:Process for the synthesis of azetidinones
发明人：THIRUVENGADAM TIRUVETTIPURAM K; FU XIAOYONG; TANN CHOU-HONG; MCALLISTER TIMOTHY L; CHIU JOHN S; COLON CESAR
权利人:SCHERING CORP
摘要:This invention provides a process for preparing the hypocholesterolemic compoundcomprising:(a) reacting p-fluorobenzoylbutyric acid with pivaloyl chloride and acylating the product with a chiral auxiliary to obtain a ketone of formula IV:(b) reducing the ketone of formula IV in the presence of a chiral catalyst to an alcohol:(c) reacting the chiral alcohol of step (b), an imine and a silyl protecting agent, then condensing the protected compounds to obtain a beta-(substituted-amino)amide of formula VII:(d) cyclizing the beta-(substituted-amino)amide of formula VII with a silylating agent and a fluoride ion catalyst to obtain a protected lactam of the formula VIII:and removing the protecting groups.The intermediates of formulas VII and VIII are also claimed.

专利号:US-5919672-A
优先权日:1998-10-02
标题 :Resolution of trans-2-(alkoxycarbonylethyl)-lactams useful in the synthesis of 1-(4-fluoro-phenyl)-3(R)- (S)-hydroxy-3-(4-fluorophenyl)-propyl!-4(S)-(4-hydroxyphenyl)-2-azetidinone
发明人：HOMANN MICHAEL J; MORGAN WILLIAM BRIAN
权利人:SCHERING CORP
摘要:A process for the microbiological or enzymatic hydrolytic resolution of racemic trans-2-(alkoxycarbonylethyl) lactams of the formula I: wherein R is C1-C7 alkyl, 2,2,2-trifluoroethyl or methoxyethoxyethyl and R1 is hydrogen or a protecting group is disclosed, whereby an optically enriched compound of the formula Ib or IIa: is obtained.

专利号:US-2005250961-A1
优先权日:2002-06-05
标题:Process for the preparation of 4-(4-fluorobenzoyl) butyric acid
发明人：PULLA REDDY M
权利人:PULLA REDDY M
摘要:The present invention provides an improved process for the preparation of 4-(4-Fluorobenzoyl)butyric acid of formula (I), which is prepared on a commercial scale using normal quality fluorobenzene (benzene content 300-700 ppm) with the desfluoro analogue impurity at an acceptable level (less than 0.1% by HPLC). The 4-(4-Fluorobenzoyl)butyric acid has the formula (I) is a key raw material for the synthesis of anti-hyperlipoproteinemetic drug ezetimibe.

专利号:EP-1137634-B1
优先权日:1998-12-07
标 题 :Process for the synthesis of azetidinones
发明人：THIRUVENGADAM TIRUVETTIPURAM K; FU XIAOYONG; TANN CHOU-HONG; MCALLISTER TIMOTHY L; CHIU JOHN S; COLON CESAR
权利人:SCHERING CORP
摘要:This invention provides a process for preparing the hypocholesterolemic compound (I) comprising: (a) reacting p-fluorobenzoylbutyric acid with pivaloyl chloride and acylating the product with a chiral auxiliary to obtain a ketone of formula (IV); (b) reducing the ketone of formula (IV) in the presence of a chiral catalyst to an alcohol; (c) reacting the chiral alcohol of step (b), an imine and a silyl protecting agent, then condensing the protected compounds to obtain a β-(substituted-amino)amide of formula (VII); (d) cyclizing the β-(substituted-amino)amide of formula (VII) with a silylating agent and a fluoride ion catalyst to obtain a protected lactam of formula (VIII); and removing the protecting groups. The intermediates of formulas (VII and VIII) are also claimed.