CAS: 24316-19-6; (1S,3Ar,14Bs)-2-Methoxy-1,5,6,8,9,14B-Hexahydro-4H-[1,3]Dioxolo[4',5':4,5]Benzo[1,2-D]Cyclopenta[b]Pyrrolo[1,2-A]Azepin-1-Ol

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CAS号38750-57-1 3-Deoxy-3-ox°Ce... | CAS号691891-10-8 (4S,5S)-1,2-did... | CAS号26833-87-4 高三尖杉酯碱 | CAS号26833-85-2 三尖杉酯碱

(+/-)-2,2-Dimethyl-3αβ,6αβ-Dihydro-4H-Cyclopenta-1,3-Dioxol-4-One置于palladium On Activated Charcoal Chromium Dichloride,盐酸,甲醇,六甲基磷酰三胺,Sodium Tetrahydroborate,Samarium Diiodide,Cerium(III) Chloride,Schwartz'S Reagent,氢气,Silver Trifluoromethanesulfonate,双(三甲基硅烷基)氨基钾,Caesium Carbonate,戴斯-马丁氧化剂,对甲苯磺酸,三乙胺,间氯过氧苯甲酸,Ytterbium(III) Triflate体系中,用 四氢呋喃,1,4-二氧六环,二氯甲烷,水,乙酸乙酯,丙酮,乙腈,叔丁醇 用作溶剂,化学反应 208.42H,反应生成三尖杉碱
参考文献:N-乙烯基-2-芳基氮丙啶的应变释放重排.抗白血病生物碱 (-)-Deoxyharringtonine 的全合成
标题:N-乙烯基-2-芳基氮丙啶的应变释放重排.抗白血病生物碱 (-)-Deoxyharringtonine 的全合成
摘要:Deoxyharringtonine (1) 是从 Cephalotaxus 属中分离出的最有效的抗白血病生物碱之一.报道了 (-)-1 的收敛全合成,涉及新的合成方法和策略,包括 (1) 用于 [3] 苯并氮杂合成的 N-芳基-2-乙烯基氮丙啶的应变释放重排,(2) 一种乙烯基酰胺用于螺-吡咯烷构建的酰化-环加成级联反应,以及 (3) α-(β-内酯) 羧酸衍生物对头孢菌素核心的有效酰化,以获得具有生物活性的头孢菌酯.这些创新不仅应允许快速获取其他三尖杉生物碱,而且还应允许快速获取具有潜在治疗效用的非天然类似物.
Doi:10.1021/ja063304F

专利信息

专利号:WO-2018019549-A1
优先权日:2016-07-28
标 题:Dioxolanone intermediate useful in the synthesis of homoharringtonine
发明人：ALLEGRINI PIETRO; CATTANEO CRISTIAN; CICERI DANIELE; GAMBINI ANDREA; PETERLONGO FEDERICO; CERISOLI LUCIA; LOMBARDO MARCO
权利人:INDENA SPA
摘要:The invention discloses 2-((2R,4R)-4-(4-(benzyloxy)-4-methylpent-2-yn-1-yl)-2-(tert-butyl)-5-oxo-1,3-dioxolan-4-yl)acetic acid of formula (XIX), a process for its preparation and processes for its conversion into enantiomerically pure (R)-2-(2-methoxy-2-oxoethyl)-6,6-dimethyltetrahydro-2H-pyran-2-carboxylic acid of formula (I), a molecule useful for the synthesis of Homoharringtonine.

专利号:US-2024287041-A1
优先权日:2021-05-20
标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms
发明人：BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN
权利人:KARYOPHARM THERAPEUTICS INC
摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.

专利号:US-3959312-A
优先权日:1974-12-20
标 题 :Synthesis of antitumor alkaloid deoxyharringtonine and its precursor 3'-0-(5-methyl-2-oxohexanoyl)-cephalotaxine
发明人：MIKOLAJCZAK KENNETH L; SMITH JR CECIL R
权利人:US AGRICULTURE
摘要:The alkaloid deoxyharringtonine and its precursor 3'-O-(5-methyl-2-oxohexanoyl)-cephalotaxine were synthesized according to the following preferred series of reactions: Ethyl t-butyl oxalate + 1-lithio-3-methylbut-1-yne -> t-butyl 5-methyl-2-oxohex-3-ynoate -> t-butyl 5-methyl-2-oxohexanoate -trifluoroacetic acid 5-methyl-2-oxohexanoic acid (COCl)+402 5-methyl-2-oxohexanoyl chloride cephalotaxine 3'-O-(5-methyl-2-oxohexanoyl)-cephalotaxine lithio methyl acetate deoxyharringtonine.

专利号:WO-02055470-A1
优先权日:2000-12-29
标 题 :Method for the enantioselective preparation of adducts of $g(a)-substituted phenylethylamine-cycloalkanes and of 2-acetoxyacrylonitrile, intermediates in the enantioselective synthesis of the lateral chain of harringtonines
发明人：DUMAS FRANCOISE; ROBIN JEAN-PIERRE; KELLER LAURENT; BATAILLE PATRICIA; D ANGELO JEAN
权利人:ONCOPHARM; CENTRE NAT RECH SCIENT; DUMAS FRANCOISE; ROBIN JEAN-PIERRE; KELLER LAURENT; BATAILLE PATRICIA; D ANGELO JEAN
摘要:The invention relates to a method for the enantioselective preparation of adducts of alpha -substituted phenylethylimino-cycloalkanes and of 2-acetoxyacrylonitrile with the formula (I), wherein the carbon atom in position 1' has the stereochemistry 1'S or 1'R; n = 0 to 3; Z is a protected alcohol radical having the formula OGP<1>; GP<1> is a protective group such as a carbon-containing ether, a silylated ether or an ester; GP<2> is a protective group of enols such as a silylated ether; and involving a Michael reaction between the methyl cyanoacetate and a chiral imine.

专利号:US-2022363662-A1
优先权日:2021-04-20
标题 :Compounds as lxr agonists
发明人：PUJALA BRAHMAM; SATHE BALAJI DASHRATH; DANODIA ABHINANDAN; GUPTA ASHU; SONI SANJEEV; KUMAR VIVEK; ANSARI AMANTULLAH; KHAN FARHA; SARKAR ARINDAM; PAYGHAN PAVAN V
权利人:INTEGRAL BIOSCIENCES PRIVATED LTD
摘要:The present invention generally discloses compounds having LXR (the liver X receptor) agonistic activity, to the use of such compounds in the treatment of various disorders such as proliferative disorders, Alzheimer's disease, inflammatory diseases, and diseases characterized by defects in cholesterol and lipid metabolism. Specifically, the present invention discloses compound of formula (IA) which exhibit LXR agonist activity, specifically to LXRβ. The invention also discloses method of synthesis of said compounds, method of using said compounds, pharmaceutical compositions comprising said compounds and method of using thereof.

专利号:AU-2022276509-A1
优先权日:2021-05-20
标题:Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms