专利号:US-10920229-B2 优先权日:2014-07-16 标 题:Method for improving heterologous synthesis of Escherichia coli into polyketides and use of same 发明人:WANG YONG; XIONG ZHIQIANG; SONG SHUJIE; LIU QIAOXIA; WANG JIANFENG 权利人:SHANGHAI INST BIOLOGICAL SCIENCES CAS; CAS CENTER FOR EXCELLENCE IN MOLECULAR PLANT SCIENCES 摘要:The present invention relates to a method for improving the heterologous synthesis of a polyketide by E. coli and use thereof. The yield of the polyketide heterologously synthesized by E. coli is significantly increased by attenuating the expression of seventy-two genes, such as sucC and talB, in a host strain, wherein the highest yield increase rate can reach 60% or more. Currently, erythromycin is the most clear model compound in the study on the biosynthesis of polyketids. The production strain of the present invention enables massive accumulation of 6-deoxyerythronolide (6-dEB), an erythromycin precursor, in the fermentation process, laying the foundation for the industrial production of the heterologous synthesis of erythromycin by E. coli.
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-12018313-B2 优先权日:2016-12-28 标题:Methods, apparatuses, and systems for microorganism strain analysis of complex heterogeneous communities with tracer analytics, determination of functional relationships and interactions thereof, and synthesis of microbial ensembles 发明人:EMBREE MALLORY 权利人:NATIVE MICROBIALS INC 摘要:Methods, apparatuses, and systems for microorganism strain analysis of complex heterogeneous communities with tracer analytics, determination of functional relationships and interactions thereof, and synthesis of microbial ensembles, including dosed microbial ensembles and inoculative microbial ensembles, are disclosed.
专利号:US-11155562-B2 优先权日:2014-06-30 标 题 :Synthesis of halichondrin analogs and uses thereof 发明人:KISHI YOSHITO; UEDA ATSUSHI; YAMAMOTO AKIHIKO; KATO DAISUKE 权利人:HARVARD COLLEGE 摘要:The present invention provides halichondrin analogs, such as compounds of Formula (I). The compounds may bind to microtubule sites, thereby inhibiting microtubule dynamics. Also provided are methods of synthesis, pharmaceutical compositions, kits, methods of treatment, and uses that involve the compounds for treatment of a proliferative disease (e.g., cancer). Compounds of the present invention are particularly useful for the treatment of metastatic breast cancer, non-small cell lung cancer, prostate cancer, and sarcoma. The included methods of synthesis are useful for the preparation of compounds of Formula (I)-(III) along with naturally occurring halicondrins (e.g., halichondrin B & C, norhalichondrin A, B, & C, and homohalichondrin A, B, & C). Also included are methods for interconverting between the halichondrins, norhalichondrins, and homohalichondrins and their unnatural epimers at the C38 ketal stereocenter through the use of an acid-mediated equilibration.
专利号:US-9328109-B2 优先权日:2013-01-14 标 题:Process for the preparation of benzohetero [1, 3] diazole compounds disubstituted with heteroaryl groups 发明人:BIANCHI GABRIELE; PO' RICCARDO 权利人:ENI SPA 摘要:Process for the preparation of a benzohetero-[1,3]diazole compound disubstituted with brominated heteroaryl groups which comprises reacting at least one dihalogenated benzohetero[1,3]diazole compound with at least one brominated heteroaryl compound. Said benzohetero[1,3]diazole compound disubstituted with brominated heteroaryl groups can be advantageously used in the synthesis of compounds useful in the construction of solar concentrators (LSCs—“Luminescent Solar Concentratorsâ€?). Furthermore, said benzohetero[1,3]diazole compound disubstituted with brominated heteroaryl groups can be advantageously used in the synthesis of photoactive polymers useful in the construction of photovoltaic devices (or solar devices) such as, for example, photovoltaic cells (or solar cells), photovoltaic modules (or solar modules), on both rigid or flexible supports. Furthermore, said benzohetero[1,3]diazole compound disubstituted with brominated heteroaryl groups can be advantageously used as precursor of monomeric units in the synthesis of semiconductr polymers.
专利号:US-9982005-B2 优先权日:2013-04-04 标 题 :Macrolides and methods of their preparation and use 发明人:MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG 权利人:HARVARD COLLEGE 摘要:Provided herein are methods of preparing macrolides by the coupling of an eastern and western half, followed by macrocyclization, to provide macrolides, including both known and novel macrolides. Intermediates in the synthesis of macrolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using the inventive macrolides are also provided. A general diastereoselective aldol methodology used in the synthesis of the western half is further provided.
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合成参考文献
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