CAS: 104987-11-3; (3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R,26As)-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26A-Hexadecahydro-5,19-Dihydroxy-3-[(1E)-2-[(1R,3R,4R)-4-Hydroxy-3-Methoxycyclohexyl]-1-Methylethenyl]-14,16-Dimethoxy-4,10,12,18-Tetramethyl-8-(2-Propen-1-yl)-15,19-E

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CAS号118977-96-1 | CAS号133941-75-0 24,32-双-O-(tert... | CAS号197250-11-6 | CAS号133951-08-3 9-deoxo FK506 | CAS号197250-10-5 | CAS号3105-95-1 L-哌啶酸 | CAS号134590-88-8 他克莫司内酯异构体 | CAS号134556-79-9 22-羟基-33-叔丁基二甲基...

他克莫司置于1,5-Diazabicyclo[4.3.0]-Non-2-Ene体系中,用 二氯甲烷 用作溶剂,以14.7%的收率获得8-表他克莫司
参考文献:Synthesis And Characterization Of An Epimer Of Tacrolimus,An Immunosuppressive Drug
标题:Synthesis And Characterization Of An Epimer Of Tacrolimus,An Immunosuppressive Drug
摘要:8-Epitacrolimus (2),A New L-Pipecolic Acid Macrolide Lactone,Was Obtained By Base-Catalyzed Epimerization Of Tacrolimus (Fk-506,1),An Important Immunosuppressive Drug,And Its Structure Determined By A Single-Crystal X-Ray Diffraction Method. The Compound Was Fully Characterized By Spectroscopic Techniques. The Epimer Is Of Importance Due To Its Potential Biological Effects As Well As Because Of Its Possible Formation During Formulation,Handling,And Use Of Tacrolimus Products.
Doi:10.1021/np9007975

专利信息

专利号:US-7230101-B1
优先权日:2002-08-28
标 题:Synthesis of methotrexate-containing heterodimeric molecules
发明人：MURTHI KRISHNA K; SMITH CHASE C
权利人:GPC BIOTECH INC
摘要:The present invention relates to novel compositions of methotrexate-containing heterodimeric probe molecules, also known as chemical inducers of dimerization (CID), useful in three-hybrid assays. The invention further relates to synthesis of said compositions and their intermediates. Another aspect of the invention is a method for using the heterodimeric probe molecules described herein in drug screens to identify potential protein targets to a given ligand, optimize protein-ligand interactions, or identify potential ligands for a given protein target. In certain embodiments, the invention contemplates the synthesis of the following methotrexate-containing heterodimeric probe:

专利号:US-2004018598-A1
优先权日:2000-05-30
标题 :Bio-intermediates for use in the chemical synthesis of polyketides
发明人：SANTI DANIEL; ASHLEY GARY; MYLES DAVID C
摘要:The present invention relates to compounds made by a subset of modules from one or more polyketide synthase (“PKSâ€?) genes that are used as starting material in the chemical synthesis of novel molecules, particularly naturally occurring polyketides or derivatives thereof. The biologically derived intermediates (“bio-intermediatesâ€?) generally represent particularly difficult compounds to synthesize using traditional chemical approaches due to one or more stereocenters. In one aspect of the invention, an intermediate in the synthesis of epothilone is provided that feeds into the synthetic protocol of Danishefsky and co-workers. In another aspect of the invention, intermediates in the synthesis of discodermolide are provided that feed into the synthetic protocol of Smith and co-workers. By taking advantage of the inherent stereochemical specificity of biological processes, the syntheses of key intermediates and thus the overall syntheses of compounds like epothilone and discodermolide are greaty simplified.

专利号:US-12221452-B2
优先权日:2017-10-04
标题:Synthesis of cantharidin
发明人：DAVIDSON MATTHEW GENE; EKLOV BRIAN MATTHEW; WUTS PETER; LOERTSCHER BRAD MELVIN; SCHOW STEVEN R
权利人:VERRICA PHARMACEUTICALS INC
摘要:The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).

专利号:US-4940797-A
优先权日:1989-03-23
标题:Process for synthesis of FK-506 C10-C18 intermediates
发明人：JONES TODD K; MILLS SANDER G; DESMOND RICHARD
权利人:MERCK & CO INC
摘要:A process is described for the improved synthesis of the optically pure C 10 -C 18 fragment of the macrolide structure of the immunosuppressant FK-506. This compound is also useful as an intermediate for preparing FK-506 derivatives.

专利号:US-9315483-B2
优先权日:2007-09-13
标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof
发明人：JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT
权利人:CONCERT PHARMACEUTICALS INC
摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.

专利号:US-5446158-A
优先权日:1989-01-11
标题:Process for synthesis of FK-506 and tricarbonyl intermediates
发明人：JONES TODD K; MILLS SANDER G; ASKIN DAVID; REAMER ROBERT A; DESMOND RICHARD; TSCHAEN DAVID M; VOLANTE RALPH P; SHINKAI ICHIRO
权利人:MERCK & CO INC
摘要:A process is described for the total synthesis of the macrolide immunosuppressant, FK-506, and important tricarbonyl process intermediates thereof. The tricarbonyl intermediates can be produced by the mild oxidation of 2,3-dihydroxy carboxylate compounds containing olefin moieties.