CAS: 186692-73-9; 4,8-Dihydroxy-5,5,7,9-Tetramethyl-16-[1-(2-Methyl-1,3-Thiazol-4-yl)Prop-1-En-2-Yl]-1-Oxacyclohexadec-13-Ene-2,6-Dione

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CAS号186692-84-2 (4S,7R,8S,9S,16... | CAS号184246-38-6 (2E)-2-Methyl-3... | CAS号187283-46-1 (3S)-2-methyl-1... | CAS号186692-68-2 (1E,3S,5Z)-2-me... | CAS号20949-84-2 2-甲基-4-噻唑甲醛 | CAS号152044-53-6 埃博霉素A | CAS号193071-75-9 [1R,3S,7S,10R,1...

📜(1E,3Z)-1-甲氧基-2-甲基-3-(三甲基硅氧基)-1,3-戊二烯置于吡啶,咪唑,2,6-二甲基吡啶,N-碘代丁二酰亚胺,Lithium Aluminium Tetrahydride,草酰氯,偶氮二异丁腈,Camphor-10-Sulfonic Acid,Diethylzinc,三正丁基氢锡,四氯化钛,双(三甲基硅烷基)氨基钾,戴斯-马丁氧化剂,对甲苯磺酸,氟化氢吡啶,二甲基亚砜,9-硼双环[3.3.1]壬烷,2,3-二氯-5,6-二氰基-1,4-苯醌,[双(三氟乙酰氧基)碘]苯体系中,用 四氢呋喃,1,4-二氧六环,乙醚,二氯甲烷,水,N,N-二甲基甲酰胺,甲苯,苯 用作溶剂,化学反应 20.75H,反应生成埃博霉素c
参考文献:Total Syntheses Of Epothilones A And B
标题:Total Syntheses Of Epothilones A And B
摘要:Convergent,Stereocontrolled Total Syntheses Of The Microtubule-Stabilizing Macrolides Epothilones A (2) And B (3) Have Been Achieved. Four Distinct Ring-Forming Strategies Were Pursued (See Scheme 1). Of These Four,Three Were Reduced To Practice. In One Approach,The Action Of A Base On A Substance Possessing An Acetate Ester And A Nonenolizable Aldehyde Brought About A Remarkably Effective Macroaldolization See (89--> 90 + 91; 99--> 100 + 101),Simultaneously Creating The C2-C3 Bond And The Hydroxyl-Bearing Stereocenter At C-3. Alternatively,The 16-Membered Macrolide Of The Epothilones Could Be Fashioned Through A C12-C13 Ring-Closing Olefin Metathesis (E.G. See 111--> 90 + 117; 122--> 105 + 123) And Through Macrolactonization Of The Appropriate Hydroxy Acid (E.G. See 88--> 93). The Application Of A Stereospecific B-Alkyl Suzuki Coupling Strategy Permitted The Establishment Of A Cis C12-C13 Olefin,Thus Setting The Stage For An Eventual Site-And Diastereoselective Epoxidation Reaction (See 96--> 2; 106--> 3). The Development Of A Novel Cyclopropane Solvolysis Strategy For Incorporating The Geminal Methyl Groups Of The Epothilones (See 39--> 40--> 41),And The Use Of Lewis Acid Catalyzed Diene-Aldehyde Cyclocondensation (Lacdac) (See 35 + 36--> 37) And Asymmetric Allylation (See 10--> 76) Methodology Are Also Noteworthy.
Doi:10.1021/ja971946K

专利信息

专利号:US-2007015260-A1
优先权日:2002-03-14
标 题:Synthesis of synthons for the manufacture of bioactive compounds
发明人：WONG CHI-HUEY; LIU JUNJIE; DESANTIS GRACE; BURK MARK
权利人:SCRIPPS RESEARCH INST
摘要:The present invention is based on the discovery that 2-deoxyribose-5-phosphate aldolase (DERA, EC 4.1.2.4) and variants thereof can be used to catalyze sequential asymmetric aldol reactions between a wide variety of donor and acceptor aldehydes. The reaction products typically contain at least two new stereogenic centers and can be produced in enantiomerically pure form. As such, DERA catalyzed asymmetric aldol chemistry can be exploited to produce synthons for the synthesis of a variety of bioactive molecules.

专利号:US-11807617-B2
优先权日:2017-05-08
标题 :Highly efficient synthesis of Z-macrocycles using stereoretentive, ruthenium-based metathesis catalysts
发明人：AHMED TONIA S; GRUBBS ROBERT H
权利人:CALIFORNIA INST OF TECHN
摘要:A highly efficient, Z-selective ring-closing metathesis system for the formation of macrocycles using a stereoretentive, ruthenium-based catalyst supported by a dithiolate ligand is reported. This catalyst is demonstrated to be remarkably active as observed in initiation experiments showing complete catalyst initiation at −20° C. within 10 min. Using easily accessible diene starting materials bearing a Z-olefin moiety, macrocyclization reactions generated products with significantly higher Z-selectivity in appreciably shorter reaction times, in higher yield, and with much lower catalyst loadings than in previously reported systems. Macrocyclic lactones ranging in size from twelve-membered to seventeen-membered rings are synthesized in moderate to high yields (68-79% yield) with excellent Z-selectivity (95%-99% Z).

专利号:US-8513429-B2
优先权日:2002-08-23
标 题:Synthesis of epothilones, intermediates thereto and analogues thereof
发明人：DANISHEFSKY SAMUEL J; RIVKIN ALEXEY; FUMIKIKO YOSHIMURA; CHOU TING-CHAO; GABARDA ANA E; DONG HUAJIN
权利人:DANISHEFSKY SAMUEL J; RIVKIN ALEXEY; FUMIKIKO YOSHIMURA; CHOU TING-CHAO; GABARDA ANA E; DONG HUAJIN; SLOAN KETTERING INSITUTE FOR CANCER RES
摘要:The present invention provides compounds of formula (I): n n n n n n n n n n n n as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (I) and provides methods of treating cancer comprising administering a compound of formula (I).

专利号:US-2005043376-A1
优先权日:1996-12-03
标题:Synthesis of epothilones, intermediates thereto, analogues and uses thereof
发明人：DANISHEFSKY SAMUEL J; BERTINATO PETER; SU DAI-SHI; MENG DONGFANG; CHOU TING-CHAO; KAMENECKA TED; SORENSEN ERIK J; BALOG AARON; SAVIN KENNETH A
摘要:The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype.

专利号:US-2023382819-A1
优先权日:2020-10-14
标 题:Processes for synthesis of alpha-emitting radiopharmaceuticals
发明人：MORSE DAVID L; WADAS THADDEUS J; PANDYA DARPAN; TAFRESHI NARGES; BUDZEVICH MIKALAI
权利人:H LEE MOFFITT CANCER CT & RES; UNIV IOWA RES FOUND
摘要:The present disclosure provides processes for the preparation of alpha emitting radiopharmaceutical compositions, in particular DOTATATE complexes of alpha emitting radionuclides, as well as use of such prepared compositions in the treatment of cancers.

专利号:US-RE41990-E
优先权日:1996-12-03
标 题 :Synthesis of epothilones, intermediates thereto, analogues and uses thereof
发明人：DANISHEFSKY SAMUEL J; BERTINATO PETER; SU DAI-SHI; MENG DONGFANG; CHOU TING-CHAO; KAMENECKA TED; SORENSEN ERIK J; BALOG AARON; SAVIN KENNETH A
权利人:SLOAN KETTERING INST CANCER
摘要:The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype.