= 83881-51-0 [标题:Reaction Conditions 标题:Process For Preparation Of Cetirizine,Its Dihydrochloride,And Optical Isomers Via Hydrolysis And Corresponding Nitriles 参考文献:United Kingdom]
2-{2-[4-[(4-氯苯基)苯基甲基]-1-哌嗪基]乙氧基}乙醛二乙基缩醛置于盐酸,Sodium Hydroxide,双氧水体系中,用 水,乙醇 作为反应溶剂,化学反应 0.5H,以85.3%的收率获得产物西替利嗪 参考文献:A Process For The Preparation Of 2-2-4-(Diphenylmethyl)-1-Piperazinyl]Ethoxy Acetic Acid Compounds Or Salts Thereof 标题:A Process For The Preparation Of 2-2-4-(Diphenylmethyl)-1-Piperazinyl]Ethoxy Acetic Acid Compounds Or Salts Thereof
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-7619085-B2 优先权日:2005-03-03 标 题 :Pyroglutamate salts and their use in the optical resolution of intermediates for the synthesis of dextrocetirizine and levocetirizine 发明人:PALACIO MAGALI; ATES CELAL 权利人:UCB PHARMA SA 摘要:The present invention relates to (S)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide-(S)-pyrrolidone-5-carboxylic acid salt; (R)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide-(S)-pyrrolidone-5-carboxylic acid salt; (S)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide-(R)-pyrrolidone-5-carboxylicacid salt; or (R)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxycetamide-(R)-pyrrolidone-5-carboxylic salt. The present invention relates also to a process for preparing (S)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide (I) and (R)-2-[4-(4-chlorobenzhydryl) piperazin-1-yl]-ethoxyacetamide (II) by chemical resolution of a mixture. These compounds are respectively intermediates for the synthesis of dextrocetirizine and levocetirizine.
专利号:US-2014275582-A1 优先权日:2013-03-14 标 题 :Chiral 2-arylpropyl-2-sulfinamide and chiral n-2-arylpropyl-2-sulfinylimines and synthesis thereof 发明人:LI GUIGEN 权利人:LI GUIGEN; UNIV TEXAS TECH; NANJING UNIVERSITY INST OF CHEMISTRY AND BIOMEDICAL SCIENCES 摘要:Provided herein are novel chiral sulfinamide and imine compounds. Also provided herein are methods of synthesizing novel chiral sulfinamide and imine compounds comprising simplified purification methods when compared to prior methods. The novel chiral sulfinamide and imine compounds are useful, for example, in the synthesis of complex natural products and pharmaceutical important compounds.
专利号:US-9216953-B2 优先权日:2012-11-02 标题 :Chiral 2-arylpropyl-2-sulfinamide and chiral N-2-arylpropyl-2-sulfinylimines and synthesis thereof 发明人:LI GUIGEN; PINDI SURESH 权利人:LI GUIGEN; PINDI SURESH 摘要:Provided herein are novel chiral sulfinamide and imine compounds. Also provided herein are methods of synthesizing novel chiral sulfinamide and imine compounds comprising simplified purification methods when compared to prior methods. The novel chiral sulfinamide and imine compounds are useful, for example, in the synthesis of complex natural products and pharmaceutical important compounds.
专利号:US-8653238-B2 优先权日:2006-02-27 标题:Compositions and methods for transport of molecules with enhanced release properties across biological barriers 发明人:WENDER PAUL A; GOUN ELENA A; JONES LISA R 权利人:WENDER PAUL A; GOUN ELENA A; JONES LISA R; UNIV LELAND STANFORD JUNIOR 摘要:Conjugates of a cargo molecule with a transporter molecule are disclosed, where the cargo molecule and the transporter molecule are linked covalently by a releasable linker. The cargo of the conjugate can be a biologically active agent or a reporter molecule. The transporter modulates the transport of the cargo across a biological barrier (e.g., a cell membrane) compared to the transport of the unconjugated cargo. Releasable linkers suitable for rapid and facile conjugation to various types of cargo and transporters are also disclosed, along with methods for using the linkers in the synthesis of conjugates.
专利号:US-6603003-B2 优先权日:2000-11-07 标 题 :Method for the preparation of piperazine and its derivatives 发明人:SEBASTIAN SONNY; PATEL HETAL VIRENDRA; THENNATI RAJAMANNAR 权利人:SUN PHARMACEUTICAL IND LTD 摘要:A novel method for the synthesis of piperazine and its derivatives of formula 1,wherein R is selected from hydrogen, or a lower alkyl group having 1 to 6 carbon atoms or a phenylalkyl group the alkyl of which has 1 to 4 carbon atoms;R1 is selected from hydrogen, a methyl group, a phenyl group optionally substituted with an alkyl group having 1 to 6 carbon atoms, or a phenylalkyl group the alkyl of which has 1 to 4 carbon atoms; andR2 is selected from hydrogen, or a methyl group, or a fluoromethyl group;comprising the steps:a. reacting an ester of formula 11 with substituted or unsubstituted ethylenediamine of formula 7 to give 3,4-dehydropiperazine-2-one and its derivatives of formula 12, wherein R, R1, R2 are as defined above and R6 is a C1 to C4 linear or branched alkyl group; andb. reacting the 3,4-dehydro-piperazine-2-one and its derivatives of formula 12 with a reducing agent to yield the piperazine and its derivatives of formula 1.
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合成参考文献
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