CAS: 77128-70-2; Fmoc-Sar-Oh

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CAS号28920-43-6 芴甲氧羰酰氯(Fm°C-Cl) | CAS号637-96-7 盐酸肌氨酸 | CAS号50-00-0 甲醛 | CAS号29022-11-5 Fm°C-甘氨酸 | CAS号18391-77-0 1-methyl-3-phen...

Fmoc-甘氨酸置于三乙基硅烷,对甲苯磺酸,三氟乙酸体系中,用 氯仿,甲苯 作为反应溶剂,化学反应 3.0H,反应生成 芴甲氧羰酰基肌氨酸
参考文献:A New Glp-1 Analogue With Prolonged Glucose-Lowering Activity In Vivo Via Backbone-Based Modification At The N-Terminus
标题:A New Glp-1 Analogue With Prolonged Glucose-Lowering Activity In Vivo Via Backbone-Based Modification At The N-Terminus
摘要:Glucagon-Like Peptide-1 (Glp-1) Is An Endogenous Insulinotropic Hormone With Wonderful Glucose-Lowering Activity. However,Its Clinical Use In Type Ii Diabetes Is Limited Due To Its Rapid Degradation At The N-Terminus By Dipeptidyl Peptidase Iv (Dpp-Iv). Among The N-Terminal Modifications Of Glp-1,Backbone-Based Modification Was Rarely Reported. Herein,We Employed Two Backbone-Based Strategies To Modify The N-Terminus Of Tglp-1. Firstly,The Amide N-Methylated Analogues 2-6 Were Designed And Synthesized To Make A Full Screening Of The N-Terminal Amide Bonds,And The Loss Of Glp-1 Receptor (Glp-1R) Activation Indicated The Importance Of Amide H-Bonds. Secondly,With Retaining The N-Terminal Amide H-Bonds,The Beta-Peptide Replacement Strategy Was Used And Analogues 7-13 Were Synthesized. By Two Rounds Of Screening,Analogue 10 Was Identified. Analogue 10 Greatly Improved The Dpp-Iv Resistance With Maintaining Good Glp-1R Activation In Vitro,And Showed Approximately A 4-Fold Prolonged Blood Glucose-Lowering Activity In Vivo In Comparison With Tglp-1. This Modification Strategy Will Benefit The Development Of Glp-1-Based Anti-Diabetic Drugs. (C) 2016 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmc.2016.01.036

专利信息

专利号:WO-9837078-A1
优先权日:1997-02-20
标题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes
发明人：DOERWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS
摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The thiophenes are prepared by reaction of a substrate-bound primary or secondary amine with a thiophosgene equivalent and reaction of the resulting intermediate with an acceptor-substituted acetonitrile in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegler-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

专利号:WO-9740025-A1
优先权日:1996-04-19
标 题 :Solid phase and combinatorial synthesis of substituted 1,2,3-triazoles and of arrays of substituted 1,2,3-triazoles
发明人：DOERWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS; DOERWALD FLORENCIO ZARAGOZA
摘要:A solid phase method for the synthesis of a plurality of differently substituted 1,2,3-triazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 1,2,3-triazoles are prepared by acylation of a substrate-bound primary or secondary amine with a 3-oxoalkanoic acid and reaction of the resulting amide with a primary amine under dehydrating conditions to give an enamine. Treatment of this substrate-bound enamine with a sulfonyl azide in the presence of a base gives the corresponding 1,2,3-triazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 1,2,3-triazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse triazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

专利号:US-6136984-A
优先权日:1996-04-22
标 题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes
发明人：DOERWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS
摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest is disclosed. The thiophenes are prepared by acylation of a substrate-bound primary or secondary amine with cyanoacetic acid and reaction of the resulting cyanoacetamide with an isothiocyanate in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegier-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

专利号:US-5847150-A
优先权日:1996-04-24
标题 :Solid phase and combinatorial synthesis of substituted 2-methylene-2, 3-dihydrothiazoles and of arrays of substituted 2-methylene-2, 3-dihydrothiazoles
发明人：DORWALD FLORENCIO ZARAGOZA
权利人:NOVO NORDISK AS
摘要:A solid phase method for the synthesis of a plurality of differently substituted 2-methylenethiazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 2-methylenethiazoles are prepared by acylation of a substrate-bound primary or secondary amine with cyanoacetic acid and reaction of the resulting cyanoacetamide with an isothiocyanate in the presence of a base. Alkylation with an appropriate alkyl halide under acidic conditions yields differently substituted, support-bound 2-methylene-2,3-dihydrothiazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 2-methylenethiazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.

专利号:US-5512668-A
优先权日:1991-03-06
标 题 :Solid phase oligonucleotide synthesis using phospholane intermediates
发明人：STEC WOJCIECH J; GRAJKOWSKI ANDRZEJ; UZNANSKI BOGDAN
权利人:POLISH ACADEMY OF SCIENCES
摘要:Methods and compounds are provided for solid phase synthesis of oligonucleotides and related polymers by condensing protected monomer-O- 1,3,2-dichalcogen-substituted-phospholane! synthons in the presence of a catalytic base. Compounds of the invention include 2-N-substituted-1,3,2-dichalcogen-substituted-phospholane precursors of the above synthons, the protected monomer-O- 1,3,2-dichalcogen-substituted-phospholane! synthons, and P-chiral oligonucleotides and related P-chiral polymers.

专利号:US-5646267-A
优先权日:1991-08-05
标 题:Method of making oligonucleotides and oligonucleotide analogs using phospholanes and enantiomerically resolved phospholane analogues
发明人：STEC WOJCIECH J; GRAJKOWSKI ANDRZEJ; UZNANSKI BOGDAN
权利人:POLISH ACADEMY OF SCIENCES
摘要:Methods and compounds are provided for solid phase synthesis of oligonucleotides and related polymers by condensing protected monomer-O-[1,3,2-dichalcogen-substituted-phospholane] synthons in the presence of a catalytic base. Compounds of the invention include 2-N-substituted-1,3,2-dichalcogen-substituted-phospholane precursors of the above synthons, the protected monomer-O-[1,3,2-dichalcogen-substituted-phospholane] synthons, and P-chiral oligonucleotides and related P-chiral polymers.