专利号:US-2023212204-A1 优先权日:2020-01-16 标题:Reagents and their use for modular enantiodivergent synthesis of c-p bonds 发明人:XU DONGMIN; RIVAS-BASCÓN NAZARET; KNOUSE KYLE W; PADIAL NATALIA; ZHENG BIN; VANTOUROUT JULIEN; SCHMIDT MICHAEL; EASTGATE MARTIN D; BARAN PHI 权利人:BRISTOL MYERS SQUIBB CO; SCRIPPS RESEARCH INST 摘要:The disclosure describes chiral P(V)-based reagents and their uses for the modular, scalable, and stereospecific synthesis of chiral phosphines, phosphine oxides and particular oligonucleotides.
专利号:US-2008045477-A1 优先权日:2001-06-15 标题 :Series Of New 4,6-Diamino-1,2-Dihydro-1-Aryl-1,3,5-Triazines, Substituted By An Adamantyl Moiety In The Position 2 Of Triazine-Their Corresponding Salts, Isomers,Steroisomers, Enantiomers, Free Bases And The Complexes Of All The Above With Natural Macromolecules And Their Synthetic Derivatives. 发明人:ANTONIADOU-VYZA EKATERINI; TSITSA POLYVXENI; ROUSSAKIS CHRISTOS 权利人:ANTONIADOU-VYZA EKATERINI; TSITSA POLYVXENI; ROUSSAKIS CHRISTOS 摘要:A series of new 4,6-diamino-1,2-dihydro-1-aryl-2-(-tricyclo[3.3.1.1 3,7 ]decyl]-1,3,5-triazines where the aryl group is a substituted or unsubstituted phenyl, or naphthyl-group, as pharmaceutically accepted salts or as free bases. The phenyl group substituents are halides, alkyls, alkoxyls or nitro group. One or more of the above substituents are found one or more times each one, and in various positions of the phenyl group. The corresponding isomers, stereoisomers, enantiomers, free bases and their complexes with various natural macromolecules and synthetic derivatives of them. The invention refers to new and prototype compounds inhibiting the proliferation of unwanted cells that belong to pathogenic microorganisms, to human tissues, to pathological cells, or any pathological cell proliferation. It also refers to the synthesis and the method of synthesis of the above mentioned compounds. The synthesis and the method of synthesis thereof of a series characterized by the preparation of the final triazines, by cyclization of the bigouanide hydrochlorides with adamantane-1-carboxaldehyde. Preparation of the inclusion complexes is realized from compexation of the corresponding hydrochlorides of the above mentioned triazines with natural macromolecules or synthetic derivatives.
专利号:US-2007015793-A1 优先权日:2003-12-23 标 题:Synthesis of nojirimycins 发明人:HIRTH BRADFORD H; RENNIE GLEN 权利人:MACROZYME DNM B V 摘要:Disclosed are methods of preparing substituted nojirimycins represented by the following formula, n n ncomprising reacting 1-deoxynojirimycin with a reagent prepared by reacting an oxidizing agent with the compound represented by the following formula.
专利号:US-2004053999-A1 优先权日:1997-09-17 标题 :Novel compounds and methods for synthesis and therapy 发明人:BISCHOFBERGER NORBERT W; DAHL TERRENCE C; HITCHCOCK MICHAEL J M; KIM CHOUNG U; LEW WILLARD; LIU HONGTAO; MILLS ROGER G; WILLIAMS MATTHEW A 摘要:Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
专利号:US-6225341-B1 优先权日:1995-02-27 标 题:Compounds and methods for synthesis and therapy 发明人:BISCHOFBERGER NORBERT W; KIM CHOUNG U; LEW WILLARD; LIU HONGTAO; WILLIAMS MATTHEW A 权利人:GILEAD SCIENCES INC 摘要:Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
专利号:WO-2014057495-A1 优先权日:2012-10-11 标 题 :A process for industrial preparation of [(s)-n-tert butoxycarbonyl-3-hydroxy]adamantylglycine 发明人:ALLA VENKAT REDDY; ALLA RAGHU MITRA; DUBEY AJAY KUMAR; REDDY P RAMAKRISHNA 权利人:LEE PHARMA LTD; ALLA VENKAT REDDY; ALLA RAGHU MITRA; DUBEY AJAY KUMAR; REDDY P RAMAKRISHNA 摘要:A commercially viable process for industrial preparation of [(S)-n-tert butoxycarbonyl-3-hydroxy]adamantylglycine which is a key intermediate for saxagliptin synthesis and is represented by compound of Formula-VI. The compound-VI obtained by the process of present invention has more than 99.5% HPLC purity, not more than 0.15 % of dihydroxy impurity, not more than 0.05% of isomer impurity and not more than 0.1% of any unknown impurity. Formula (VI).
参考标题:An Expedient Route For The Reduction Of Carboxylic Acids To Alcohols Employing 1-Propanephosphonic Acid Cyclic Anhydride As Acid Activator 作者:G. Nagendra,C. Madhu,T.M. Vishwanatha,Vommina V. Sureshbabu |发布日期:2012.9 摘要:Method For The Synthesis Of Alcohols From The Corresponding Carboxylic Acids Is Described. Activation Of Carboxylic Acid With 1-Propanephosphonic Acid Cyclic Anhydride (T3P) And Subsequent Reduction Using Nabh4 Yield The Alcohol In Excellent Yields With Good Purity. Reduction Of Several Alkyl/aryl Carboxylic Acids And Nα-Protected Amino Acids/peptide Acids As Well As Nβ-Protected Amino Acids Was Successfully
合成参考文献
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