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对甲苯磺酰甘氨酸甲酯置于lithium Hydroxide Monohydrate体系中,用 四氢呋喃,甲醇 用作溶剂,化学反应 2.0H,反应生成N-对甲苯磺酰甘氨酸
参考文献:Identification Of Bidentate Salicylic Acid Inhibitors Of Ptp1B
标题:Identification Of Bidentate Salicylic Acid Inhibitors Of Ptp1B
摘要:Ptp1B Is A Master Regulator In The Insulin And Leptin Metabolic Pathways. Hyper-Activated Ptp1B Results In Insulin Resistance And Is Viewed As A Key Factor In The Onset Of Type Ii Diabetes And Obesity. Moreover,Inhibition Of Ptp1B Expression In Cancer Cells Dramatically Inhibits Cell Growth In Vitro And In Vivo. Herein,We Report The Computationally Guided Optimization Of A Salicylic Acid-Based Ptp1B Inhibitor 6,Identifying New And More Potent Bidentate Ptp1B Inhibitors,Such As 20H,Which Exhibited A > 4-Fold Improvement In Activity. In Cho-Ir Cells,20F,20H,And 20J Suppressed Ptp1B Activity And Restored Insulin Receptor Phosphorylation Levels. Notably,20F,Which Displayed A 5-Fold Selectivity For Ptp1B Over The Closely Related Ptp Sigma Protein,Showed No Inhibition Of Ptp-Lar,Prl2 A/s,Mkpx,Or Papain. Finally,20I And 20J Displayed Nanomolar Inhibition Of Ptp Sigma,Representing Interesting Lead Compounds For Further Investigation.
Doi:10.1021/acsmedchemlett.5B00171

专利信息

专利号:US-10464958-B2
优先权日:2012-07-17
标题 :Method for the synthesis of alpha-aminoalkylenephosphonic acid
发明人：NOTTE PATRICK; COGELS SAMUEL; BURCK SEBASTIAN
权利人:MONSANTO TECHNOLOGY LLC
摘要:The present invention is related to a new method for the synthesis of alpha-aminoalkylenephosphonic acid or its phosphonate esters comprising the steps of forming a reaction mixture by mixing a P—O—P anhydride moiety comprising compound, having one P-atom at the oxidation state (+III) and the other P-atom at the oxidation state (+III) or (+V), an aminoalkanecarboxylic acid and an acid catalyst, wherein said reaction mixture comprises an equivalent ratio of alpha-aminoalkylene carboxylic acid to P—O—P anhydride moieties of at least 0.2, and recovering the resulting alpha-aminoalkylene phosphonic acid compound or an ester thereof from the reaction mixture.

专利号:US-2018346497-A1
优先权日:2012-07-17
标 题:Method for the synthesis of alpha-aminoalkylenephosphonic acid

专利号:US-2007099915-A1
优先权日:2005-10-07
标题 :Inhibitors of the hiv integrase enzyme
发明人：DRESS KLAUS R; JOHNSON TED W; PLEWE MICHAEL B; TANIS STEVEN P; ZHU HUICHUN
权利人:PFIZER
摘要:The present invention is directed to compounds of formula (I), n nand pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus (“HIVâ€?) integrase enzyme.

专利号:US-9217012-B2
优先权日:2009-04-08
标题 :Inhibitors of protein tyrosine phosphatases
发明人：ZHANG ZHONG-YIN; ZHANG SHENG
权利人:ZHANG ZHONG-YIN; ZHANG SHENG; UNIV INDIANA RES & TECH CORP
摘要:Disclosed herein are compounds that selectively inhibit members of the PTP family of enzymes. Synthesized compounds demonstrated selective inhibition of TC-PTP. Also provided are methods of using the compounds and formulations containing the compounds. Also described is a fluorescence-tagged combinatorial library synthesis and screening method. And methods of using these compounds to effect enzyme activity both in cells and in vitro as well as method of using these compounds to treat diseases in human and animals.

专利号:WO-2014012990-A1
优先权日:2012-07-17
标题:Method for the synthesis of alpha-aminoalkylenephosphonic acid

专利号:SU-1502572-A1
优先权日:1987-11-26
标题:2-(n-toluenesulfonyl)-1,2,3,4-tetrahydropyrasin (1, 2-a)-benzimidasol as intermediate product in the synthesis of 2-substituted 1,2,3,4-tetrahydropyrasin (1, 2-a)-benzimidasols, possessing biological activity