苯酚置于cocl2体系中,用 三苯基膦 用作溶剂,以91.5%的收率获得氯甲酸苯酯 参考文献:Process For The Preparation Of Chloroformic Acid Aryl Esters 标题:Process For The Preparation Of Chloroformic Acid Aryl Esters 摘要:在一种制备芳香族氯甲酸酯的过程中,通过接触苯酚和光气的改进方式,在有机磷化合物的存在下,在60oc至180oc的温度下在均相液相中进行反应,该有机磷化合物的化学式为r1R2R3Pr4Nxn,其中r1,R2和r3独立地表示氢,烷基,烯基,芳基烷基,芳基或卤素,其中两个所述基团与磷原子一起可以形成一个5元或6元含磷饱和或不饱和杂环基团,X表示oh,同极键结合的卤素或无机或有机酸根离子,R4表示氢或烷基,或者如果x表示卤素,则还可以表示卤素,N表示0或1,此外,R4和x还可以一起表示氧或硫.
专利号:US-8350031-B2 优先权日:2008-06-02 标 题:Processes for the synthesis of levocetirizine and intermediates for use therein 发明人:RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI; CHIKHALIKAR SANDIP VASANT 权利人:CIPLA LTD; RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI; CHIKHALIKAR SANDIP VASANT 摘要:The present invention provides a compound of formula (IV) n nwherein R is Cl, Br, NO 2 , OH or OR′, and R′ is alkyl, and its use in the synthesis of levocetirizine, including its use in the synthesis of (−)-1-[(4-chlorophenyl)-phenylmethyl]piperazine, an intermediate useful in the synthesis of levocetirizine. The present invention also provides compounds (II) and (III) which are useful in the synthesis of compound (IV).
专利号:US-5283293-A 优先权日:1990-12-14 标 题:Reagents for automated synthesis of peptide analogs 发明人:WEBB THOMAS R 权利人:CORVAS INC 摘要:Reagents suitable for synthesis of peptide analogs using automated peptide synthesis and procedures for synthesis of peptide analogs are provided.
专利号:US-7872143-B2 优先权日:2007-06-11 标题 :Facile synthesis of a series of liquid crystalline 2-(4′-alkoxyphenyl)-5-cyanopyridines 发明人:CHIA WIN-LONG; CHENG YU-WEI 权利人:UNIV FU JEN CATHOLIC 摘要:The invention relates to a facile synthesis of a series of 2-(4′-alkoxyphenyl)-5-cyanopyridine liquid crystal compounds which are represented by the following formula (I): n n n n n n n n n n wherein C n H 2n+1 is a linear alkyl group having 2-12 carbon atoms. The synthesis of the liquid crystalline 2-(4′-alkoxyphenyl)-5-cyanopyridine is completed in a two-step reaction. First, a Grignard reagent (such as 4-alkoxyphenylmagnesium bromide) is added to a 3-cyanopyridinium salt (such as N-phenyloxycarbonyl-3-cyanopyridinium chloride) to get a 1,2-dihydropyridine. Then, the 1,2-dihydropyridine is oxidized with o-chloronil to obtain the 2-(4′-alkoxyphenyl)-5-cyanopyridine.
专利号:US-9708317-B2 优先权日:2013-11-25 标 题 :Process for the preparation of 8-(4-aminophenoxy)-4H-pyrido[2,3-B]pyrazin-3-one derivatives 发明人:ZAMBON ALFONSO; NICULESCU-DUVAZ DAN; CHUBB RICHARD; SPRINGER CAROLINE JOY 权利人:CANCER RES TECH LTD; INST OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE); OXY SCIENT LTD; THE INST OF CANCER RESEARCH: ROYAL CANCER HOSPITAL 摘要:The present invention pertains generally to the field of organic chemical synthesis, and in particular to certain methods for the synthesis of 8-(4-aminophenyoxy)-4H-pyrido[2,3-b]pyrazin-3-one and related compounds (denoted herein as (3)) from 4-(4-aminophenyoxy)pyridine-2,3-diamine and related compounds (denoted herein as (1)), by reaction with glyoxylic acid (denoted herein as (2)). The compounds (3) are useful in the synthesis of known anti-cancer agents, such as 1-(5-tert-butyl-2-(4-methyl-phenyl)-pyrazol-3-yl)-3-[2-fluoro-4-[(3-oxo-4H-pyrido[2,3-b]pyrazin-8-yl)oxy]phenyl]urea.
专利号:US-3978084-A 优先权日:1973-12-03 标题 :Synthesis of biotin 发明人:CONFALONE PASQUALE NICHOLAS; USKOKOVIC MILAN RADOJE; PIZZOLATO GIACOMO 权利人:HOFFMANN LA ROCHE 摘要:Synthesis of biotin from 4-carbomethoxy-2-(4,5-dihydrothiophen-3(2H)-one)-valeric acid methyl ester, and thiophene intermediates in this synthesis.
专利号:US-3979396-A 优先权日:1973-12-03 标 题 :Synthesis of biotin 发明人:CONFALONE PASQUALE NICHOLAS; USKOKOVIC MILAN RADOJE; PIZZOLATO GIACOMO 权利人:HOFFMANN LA ROCHE 摘要:Synthesis of biotin from 4-carbomethoxy-2-(4,5-dihydrothiophen-3(2H)-one)-valeric acid methyl ester, and dihydrothiophene intermediates in this synthesis.