CAS: 538-60-3; Dibenzyl Hydrogen Phosphite

上下游产品

benzyl alcohol 1.3-butanediol tribenzyl phosphite Dibenzyl N,N-diisopropylphosphoramidited]thiazol-2-yl]-phosphonic acid dibenzyl ester[3-(4-amino-2-methyl-pyrimidin-5-ylmethyl)-3a-methyl-hexahydro-furo[2,3-d]thiazol-2-yl]-phosphonic acid dibenzyl ester d]thiazolo[3,4-a]pyrimidin-7-yl]-phosphonic acid dibenzyl ester[9-(2-hydroxy-ethyl)-2,9a-dimethyl-5,9,9a,10-tetrahydro-pyrimido[4,5-d]thiazolo[3,4-a]pyrimidin-7-yl]-phosphonic acid dibenzyl ester dibenzyl phosph°Chloridate dibenzyl hydroxymethylphosphonate

📜苯甲醇置于n,N-二甲基苯胺,三氯化磷体系中,用 甲苯 作为反应溶剂,化学反应生成 亚磷酸二苄酯
参考文献:Synthesis,Evaluation,And Mechanism Study Of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization In Vitro And In Vivo
标题:Synthesis,Evaluation,And Mechanism Study Of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization In Vitro And In Vivo
摘要:Twenty-Nine Novel Indole-Chalcone Derivatives Were Synthesized And Evaluated For Antiproliferative Activity. Among Them,14K Exhibited Most Potent Activity,With Ic50 Values Of 3-9 Nm Against Six Cancer Cells,Which Displayed A 3.8-8.7-Fold Increase In Activity When Compare With Compound 2. Further Investigation Revealed 14K Was A Novel Tubulin Polymerization Inhibitor Binding To The Colchicine Site. Its Low Cytotoxicity Toward Normal Human Cells And Nearly Equally Potent Activity Against Drug Resistant Cells Revealed The Possibility For Cancer Therapy. Cellular Mechanism Studies Elucidated 14K Arrests Cell Cycle At G(2)/m Phase And Induces Apoptosis Along With The Decrease Of Mitochondrial Membrane Potential. Furthermore,Good Metabolic Stability Of 14K Was Observed In Mouse Liver Microsomes. Importantly,14K And Its Phosphate Salt 14K-P Inhibited Tumor Growth In Xenograft Models In Vivo Without Apparent Toxicity,Which Was Better Than The Reference Compound Ca-4P And 2. In Summary,14K Deserves Consideration For Cancer Therapy.
DOI:10.1021/acs.Jmedchem.6B00021

专利信息

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:WO-02085848-A8
优先权日:2001-04-18
标 题 :Synthesis of pancratistatin prodrugs
发明人：PETIT GEORGE R; ORR BRIAN; DUCKI SYLVIE
权利人:UNIV ARIZONA STATE; PETIT GEORGE R; ORR BRIAN; DUCKI SYLVIE
摘要:A new and efficient synthesis of the (+)-pancratistatin phosphate prodrug 2a has been accomplished. Selective protection (tetraacetate 4) of (+)-pancratistatin (1a) 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 (2a). Further increases in yields of the prodrug (2a) were realized by avoiding heat in the final purification steps. Fourteen (2b-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:EP-0150883-B1
优先权日:1984-02-02
标题 :Process for preparing n-(dibenzyloxyphosphoryl)-cyanamide and processes using said compounds as intermediate for the synthesis of phosphagen substances
摘要:The invention relates to a process for preparing compounds of general formula: wherein R = Hydrogen, halogen, alkyl, nitro-group; said compounds, which are indicated hereinunder with the general term <> are useful as intermediates in the synthesis of phosphagen compounds such as phosphocreatine, phosphocreatinine and similar compounds. Such process is characterized in that dibenzyloxyphosphoryl chloride is reacted with cyanamide, N-(dibenzyloxyphosphoryl)-cyanamide being produced; this latter can react with substances provided with a primary or secondary amine function, to give the corresponding guanidinoderivatives; e.g., with a sarcosine derivative to give N-(dibenzyloxyphosphoryl)-creatine or N-(dibenzyloxyphosphoryl)-creatinine.

专利号:US-8785629-B2
优先权日:2009-06-18
标题 :Phosphonates synthons for the synthesis of phosphonates derivatives showing better bioavailability
发明人：AGROFOGLIO LUIGI A; ROY VINCENT; PRADERE UGO
权利人:AGROFOGLIO LUIGI A; ROY VINCENT; PRADERE UGO; CENTRE NAT RECH SCIENT; UNIV ORLEANS
摘要:Synthons for the synthesis of phosphonates prodrugs POM and POC, especially for direct Cross Metathesis.

专利号:US-11744150-B2
优先权日:2012-01-20
标 题:Synthesis of aza-acenes as novel n-type materials for organic electronics
发明人：THOMPSON MARK E; SOMMER JONATHAN R; BARTYNSKI ANDREW
权利人:UNIV SOUTHERN CALIFORNIA
摘要:Acenes, such as aza-acenes are attractive materials for organic semiconductors, specifically for n-type materials. There are disclosed new derivatives of acenes that are fabricated using novel synthesis. For example, the disclosed fabrication strategies have allowed for the first time new aza-tetracene and aza-pentacene derivatives. The HOMO and LUMO energy levels of these materials are tunable through appropriate substitution and as predicted, deepened. There are also disclosed organic photosensitive devices comprising at least one aza-acene such as aza-tetracene and aza-pentacene.