苄硫醇置于n-氯代丁二酰亚胺,三苯基膦体系中,用 二氯甲烷 用作溶剂,以70%的收率获得氯化苄 参考文献:A Facile Conversion Of Thiols To Alkyl Halides By Triphenylphosphine/n-Halosuccinimides 标题:A Facile Conversion Of Thiols To Alkyl Halides By Triphenylphosphine/n-Halosuccinimides 摘要:在室温下,使用三苯基膦/n-卤代苏氨酸酯(卤素:Br,Cl和i)在二氯甲烷中处理硫醇,能高效地将其转化为烷基卤化物,产率高至非常好. Doi:10.1055/s-2001-15157
专利信息
专利号:US-8822702-B2 优先权日:2002-12-20 标 题 :Synthesis of amines and intermediates for the synthesis thereof 发明人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL 权利人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL; BASF SE 摘要:The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, n nor especially of amides of the formula II,n n nwherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.
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-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:WO-9312076-A1 优先权日:1991-12-13 标题:Reagents for automated synthesis of peptide analogs 发明人:WEBB THOMAS ROY 权利人:CORVAS INT 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-2004058888-A1 优先权日:2000-01-13 标题:Methods for synthesis of alpha-d-gal (1~>3) gal-containing oligosaccharides 发明人:BORNAGHI LAURENT; DEKANY GYULA; DRINNAN NICHOLAS BARRY; PAPAGEORGIOU JOHN; WEST MICHAEL LEO 摘要:This invention relates to reagents and methods for synthesis of biologically active di- and tri-saccharides comprising α-D-Gal(1→3)-D-Gal. In particular the invention provides novel reagents, intermediates and processes for the solution or solid phase synthesis of α-D-galactopyranosyl-(1→3)-D-galactose, and derivatives thereof. In one preferred embodiments the invention provides a protected monosaccharide building block of general formula (II): in which R 3 is methoxy or methyl; R 1 is H, benzoyl, pivaloyl, 4-chlorobenzoyl, acetyl, chloroacetyl, levulinoyl, 4-methylbenzoyl, benzyl, 3,4-methylenedioxybenzyl, 4-methoxybenzyl, 4-chlorobenzyl, 4-acetamidobenzyl, or 4-azidobenzyl; and R 2 is H, Fmoc, benzoyl, pivaloyl, 4-chlorobenzoyl, acetyl, chloroacetyl, levulinoyl, 4-methylbenzoyl, benzyl, 3,4-methylenedioxybenzyl, 4-methoxybenzyl, 4 -chlorobenzyl, 4-acetamidobenzyl, or 4-azidobenzyl.
专利号:US-11912654-B2 优先权日:2021-09-03 标 题:Process for stereospecific synthesis of vitamin K2 and its novel intermediates 发明人:MEHTA DILIP; SHASHTRI MAYANK; RAJU BNS; SHAH ASHWIN; VORA PARIN; MAHALE UMAKANT 权利人:SYNERGIA LIFE SCIENCES PVT LTD 摘要:The present disclosure relates to a novel process for the synthesis of stereospecific compounds of Vitamin K2 group in general and Vitamin K2-7. The present disclosure further discloses novel intermediates useful in the synthesis of stereospecific Vitamin K2-7. Compounds of the Vitamin K2 group obtained are crystalline and exhibit well defined melting points.
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合成参考文献
参考文献:10.1107/s1600536811007823 摘要:Yu CX, Zhu YL, Chen ZX, Lu MZ, Wang K. 4,4',5,5'-Tetra-kis(benzyl-sulfan-yl)tetra-thia-fulvalene. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o821. 参考文献:10.1107/s1600536811011597 摘要:Ju ZY, Jiang WX, Yang FL. 2-Benzyl-6-benz-yloxypyridazin-3(2H)-one. Acta Crystallogr Sect E Struct Rep Online. 2011 May 01;67(Pt 5):o1042. 参考文献:10.1107/s1600536811015637 摘要:Fun HK, Asik SI, Razak IA, Nithinchandra, Kalluraya B. 7-(4-Chloro-benzyl-idene)-3-[(4-chloro-phen-oxy)meth-yl]-6-(4-nitro-thio-phen-2-yl)-7H-1,2,4-triazolo[3,4-b][1,3,4]thia-diazine. Acta Crystallogr Sect E Struct Rep Online. 2011 May 01;67(Pt 5):o1266–7. 参考文献:10.1107/s1600536811015686 摘要:Keng TC, Lo KM, Ng SW. (2,2′-Bipyridine-κ2N,N′)dichloridobis(4-fluorobenzyl)tin(IV). Acta Crystallogr E Struct Rep Online. 2011 May 07;67(6):m658. doi: 10.1107/s1600536811015686. 参考文献:10.1107/s1600536811015698 摘要:Keng TC, Lo KM, Ng SW. Trichlorido(4-methylbenzyl)bis(1H-pyrazole-κN2)tin(IV). Acta Crystallogr E Struct Rep Online. 2011 May 07;67(6):m659. doi: 10.1107/s1600536811015698.