专利号:US-6316593-B1 优先权日:1996-02-09 标题:Synthesis of VIP analog 发明人:BOLIN DAVID ROBERT; DANHO WALEED; FELIX ARTHUR M 权利人:HOFFMANN LA ROCHE 摘要:This invention relates to a novel process for the synthesis of vasoactive intestinal peptide analog Ac(1-31)-NH2 from four protected peptide fragments.
专利号:EP-1383732-B1 优先权日:2001-05-04 标题:Labelling reagents, method for synthesis of said reagents and methods for detecting biological molecules 发明人:BOURGET CECILE; LHOMME JEAN; LAAYOUN ALI; KOTERA MITSUHARU; TREVISIOL EMMANUELLE; MENOU LIONEL; BERNAL MENDEZ ELOY 权利人:BIO MERIEUX; UNIV GRENOBLE 1; CENTRE NAT RECH SCIENT 摘要:The invention concerns a temperature-stable labelling reagent of formula (I), wherein: R<1> represents H or an alkyl, aryl or substituted aryl group; R<2> represents a detectable marker or at least two detectable markers linked together by at least a multimeric structure; L is a linking arm comprising a linear catemer concatenation of at least two covalent bonds; and n is an integer equal to 0 or 1; R<3> and R<4> represent, independently of each other: H, NO2, Cl, Br, F, I, R<2>-(L)n-Y-X-, OR, SR, NR2, R, NHCOR, CONHR, COOR with R = alkyl or aryl, A is a linking arm comprising at least a double bond enabling the conjugation of the diazo function with the aromatic cycle; and u is a whole number between 0 and 2, preferably between 0 and 1; and -Y-X- represents -CONH-, -NHCO-, -CH2O-, -CH2S-. The invention also concerns a method for the synthesis of said markers and uses for labelling biological molecules, in particular nucleic acids, with a labelling reagent bearing the diazomethyl function. The invention is particularly applicable in the field of diagnosis.
专利号:US-9359333-B2 优先权日:2013-01-14 标 题 :Efficient process for the preparation of Lapatinib and salts thereof by means of new intermediates 发明人:FONTANA FRANCESCO; PAIO ALFREDO 权利人:F I S —FABBRICA ITALIANA SINT S P A; F I S —FABBRICA ITALIANA SINT 摘要:The present invention refers to a new efficient process for the synthesis of the active pharmaceutical ingredient Lapatinib and salts thereof. n In particular, the present synthesis is carried out employing new intermediates in which the amine function is protected by a group cleavable in basic milieu that provides a higher overall yield of the synthesis process.
专利号:US-5233044-A 优先权日:1989-06-08 标题:Active esters for solid phase peptide synthesis 发明人:HUDSON DEREK 权利人:MILLIPORE CORP 摘要:Derivatives of 1-phenyl pyrazolin-5-one have many applications for biomolecule synthesis. Enol esters of protected amino acids made by the present process provide efficient coupling in solid-phase peptide synthesis. The 1-phenyl-pyrazolin-5-one derivatives are highly crystalline, stable, non-toxic and easy to prepare. Many possess self-indicating properties, facilitating spectrophotometric monitoring and automation of peptide synthesis.
专利号:EP-0401797-A1 优先权日:1989-06-08 标 题:Active esters for solid phase peptide synthesis 发明人:HUDSON DEREK 权利人:MILLIPORE CORP 摘要:Derivatives of 1-phenyl pyrazolin-5-one have many applications for biomolecule synthesis. Enol esters of protected amino acids made by the present process provide efficient coupling in solid-phase peptide synthesis. The 1-phenyl-pyrazolin-5-one derivatives are highly crystalÂline, stable, non-toxic and easy to prepare. Many possess self-indicating properties, facilitating spectroÂphotometric monitoring and automation of peptide synthesis.
专利号:US-5861351-A 优先权日:1993-04-05 标 题:Automated allyl deprotection in solid-phase synthesis 发明人:ALBERICIO FERNANDO; KATES STEVEN A 权利人:PERSEPTIVE BIOSYSTEMS INC 摘要:A method for removing an allyl protecting group from an allyl-protected derivative of a biologically relevant amino acid is disclosed. One relevant aspect of the method is the use of soluble organometallic catalyst, such as an organopalladium catalyst. Preferably, soluble tetrakistriphenylphosphine palladium (0) is used. The allyl deprotection method now disclosed is suitable for use on an instrument for automated peptide synthesis. Methods of preparing the soluble organometallic catalyst are also disclosed, as are soluble catalyst compositions.
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合成参考文献
摘要:Albero, J.; García, H., Science of Synthesis: Photocatalysis in Organic Synthesis, (2018) 1, 583.