专利号:US-9994526-B2 优先权日:2011-04-04 标 题 :Process intermediates and methods for the preparation of process intermediates for the synthesis of argatroban monohydrate 发明人:STIVANELLO MARIANO; HUBER FLORIAN ANTON MARTIN; RICCI ANTONIO 权利人:LUNDBECK PHARMACEUTICALS ITALY S P A 摘要:Methods are provided for the synthesis of key intermediates for the synthesis of Argatroban monohydrate, ethyl (2R,4R)-1-[(2S)-2-amino-5-[[imino(nitroamino)methyl]amino]-1-oxopentyl]-4-methylpiperidine-2-carboxylate compounded with HCl. Such intermediates are also provided.
专利号:US-6251689-B1 优先权日:1998-05-14 标 题:Methods for the solid phase synthesis of combinatorial libraries of benzimidazoles benzoxazoles benzothiazoles and derivatives thereof 发明人:LABORDE EDGARDO; MATSUMOTO YUKIHARU 权利人:TELIK INC 摘要:The present invention provides an efficient and versatile method for the synthesis and screening of combinatorial libraries of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof. In order to expedite the synthesis of large arrays of compounds possessing these core structures, a general methodology for solid phase synthesis of these derivatives is provided. Arrays of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antiviral, antimicrobial, anticoagulant, and antiulcer activity, or use in the treatment of inflammation, hypertension, cancer, and other conditions can be prepared by this method.
专利号:US-6048975-A 优先权日:1991-09-12 标 题:Process for the chemical synthesis of oligonucleotides 发明人:PFLEIDERER WOLFGANG; BERGMANN FRANK 权利人:HOECHST AG 摘要:A process for the chemical synthesis of oligonucleotides n Use of a dansylethoxycarbonyl group as base-labile 5'-hydroxyl protective group in the chemical synthesis of DNA and RNA and suitable synthetic processes. n The ease of detection of the dansyl protective group and the ease of elimination from the sugar residue of the nucleotide without side reactions make oligonucleotide synthesis possible with high yields in very small quantities.
专利号:US-5945524-A 优先权日:1990-09-14 标 题 :Process for the chemical synthesis of oligonucleotides 发明人:PFLEIDERER WOLFGANG; BERGMANN FRANK 权利人:HOECHST AG 摘要:Use of a dansylethoxycarbonyl group as base-labile 5'-hydroxyl protective group in the chemical synthesis of DNA and RNA and suitable synthetic processes. n The ease of detection of the dansyl protective group and the ease of elimination from the sugar residue of the nucleotide without side reactions make oligonucleotide synthesis possible with high yields in very small quantities.
专利号:US-2003049619-A1 优先权日:2001-03-21 标题 :Methods for the synthesis of polynucleotides and combinatorial libraries of polynucleotides 发明人:DELAGRAVE SIMON; MARRS BARRY 摘要:Methods for the synthesis of polynucleotides and derivatives thereof are provided. Methods for the preparation of combinatorial libraries of polynucleotides are also provided. In addition, methods for the preparation and identification of polynucleotides having a predetermined property are provided.
专利号:US-11613514-B2 优先权日:2016-03-25 标题:Crystal forms and methods of synthesis of (2R, 6R)-hydroxynorketamine and (2S, 6S)-hydroxynorketamine 发明人:THOMAS CRAIG; ZARATE CARLOS; MOADDEL RUIN; GOULD TODD; ZANOS PANOS; MORRIS PATRICK 权利人:US HEALTH; UNIV MARYLAND 摘要:The disclosure provides a method for synthesizing free base forms of (2R,6R)-hydroxynorketamine (HNK) and (2S,6S)-hydroxynorketamine. In an embodiment synthesis of (2R,6R)-hydroxynorketamine (HNK) includes preparation of (R)-norketamine via chiral resolution from racemic norketamine via a chiral resolution with L-pyroglutamic acid. The disclosure also provided crystal forms of the corresponding (2R,6R)-hydroxynorketamine (HNK) and (2S,6S)-hydroxynorketamine hydrochloride salts.