专利号:US-2020010502-A1 优先权日:2018-07-05 标题 :Synthesis of multiphosphorylated peptides 发明人:FRIEDLER ASSAF; MAMDI SAMARA SIMHA REDDY; HUREVICH MATTAN 权利人:YISSUM RES DEV CO OF HEBREW UNIV JERUSALEM LTD 摘要:The present invention relates to a new approach for the synthesis of multiphosphorylated peptides. Specifically, the present invention provides a process, which enables the synthesis of multiphosphorylated peptides with up to seven phosphorylated Serine (pSer) and Threonine (pThr) residues, including such residues that are close in sequence.
专利号:US-2004127467-A1 优先权日:2002-04-17 标 题:Synthesis of pancratistatin prodrugs 发明人:PETTIT GEORGE R; ORR BRIAN; DUCKI SYLVIE 摘要:A new and efficient synthesis of the (+)-pancratistatin phosphate prodrug 2 a has been accomplished. Selective protection (tetraacetate 4 ) of (+)-pancratistatin ( 1 a ) was followed by phosphorylation (to 5 ) with dibenzyl chlorophosphite (prepared in situ from dibenzyl phosphite). Cleavage of the acetate (with sodium methoxide) and benzyl (by hydrogenolysis) protecting groups followed by concomitant reaction with two equivalents of sodium methoxide afforded good yield of disodium (+)-pancratistatin phosphate ( 2 a ). Further increases in yields of the prodrug ( 2 a ) were realized by avoiding heat in the final purification steps. Fourteen ( 2 b - o ) additional metal and ammonium derived phosphate prodrugs were also synthesized.
专利号:US-7105695-B2 优先权日:2001-12-21 标题 :Synthesis of combretastatin A-2 prodrugs 发明人:PETTIT GEORGE R; MOSER BRYAN R 权利人:UNIV ARIZONA STATE 摘要:The original synthesis of combretastatin A-2 (1a) was modified to provide an efficient scale-up procedure for obtaining this antineoplastic stilbene. Subsequent conversion to a useful prodrug was accomplished by phosphorylation employing in situ formation of dibenzylchlorophosphite followed by cleavage of the benzyl ester protective groups with bromotrimethylsilane to afford phosphoric acid intermediate 11. The latter was immediately treated with sodium methoxide to complete a practical route to the disodium phosphate prodrug (2a). The phosphoric acid precursor (11) of phosphate 2a was employed in a parallel series of reactions to produce a selection of metal and ammonium cation prodrug candidates. Each of the phosphate salts (2a–q) was evaluated with respect to relative solubility behavior, cancer cell growth inhibition, and antimicrobial activity.
专利号:US-12006315-B2 优先权日:2022-03-25 标题 :Intermediate useful for the synthesis of TGF-beta inhibitors and a method of preparing TGF-beta inhibitors using the same 发明人:LEE SEUNG HO 权利人:MEDPACTO INC 摘要:The present invention provides an intermediate for synthesizing a TGF-β inhibitor represented by Chemical Formula 1 and an improved method for preparing the TGF-β inhibitor represented by Chemical Formula 1 using the same. The preparation method according to the present invention can not only allow inexpensive and safe reagents to be used, but also simplify the synthesis steps and purification methods to improve the reaction yield, thereby maximizing the production efficiency of the TGF-β inhibitor represented by Chemical Formula 1 to be used usefully for mass production.
专利号:US-6319695-B1 优先权日:1991-10-15 标 题:Production of fucosylated carbohydrates by enzymatic fucosylation synthesis of sugar nucleotides; and in situ regeneration of GDP-fucose 发明人:WONG CHI-HUEY; ICHIKAWA YOSHITAKA; SHEN GWO-JENN; LIU KUN-CHIN 权利人:SCRIPPS RES INSITUTE 摘要:This invention contemplates improved methods of enzymatic production of carbohydrates especially fucosylated carbohydrates. Improved syntheses of glycosyl 1- or 2-phosphates using both chemical and enzymatic means are also contemplated. The phosphorylated glycosides are then used to produce sugar nucleotides that are in turn used as donor sugars for glycosylation of acceptor carbohydrates. Especially preferred herein is the use of a disclosed method for fucosylation.
专利号:US-7335500-B2 优先权日:1991-10-15 标 题:Production of fucosylated carbohydrates by enzymatic fucosylation synthesis of sugar nucleotides; and in situ regeneration of GDP-fucose 发明人:WONG CHI-HUEY; ICHIKAWA YOSHITAKA; SHEN GWO-JENN; LIU KUN-CHIN 权利人:SCRIPPS RESEARCH INST 摘要:This invention contemplates improved methods of enzymatic production of carbohydrates especially fucosylated carbohydrates. Improved syntheses of glycosyl 1- or 2-phosphates using both chemical and enzymatic means are also contemplated. The phosphorylated glycosides are then used to produce sugar nucleotides that are in turn used as donor sugars for glycosylation of acceptor carbohydrates. Especially preferred herein is the use of a disclosed method for fucosylation.
[参考文献]: Yulia Kaluzhny, Et Al. The Epiocular Eye Irritation Test (Eit) For Hazard Identification And Labelling Of Eye Irritating Chemicals: Protocol Optimisation For Solid Materials And The Results After Extended Shipment. Altern Lab Anim. 2015 May;43(2):101-27.
合成参考文献
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