专利号:US-3947517-A 优先权日:1969-06-12 标题:Stereoselective introduction of tetracyclines hydroxyl group at 12(a) position in synthesis of tetracyclines 发明人:MUXFELDT HANS H; MICHAEL JEFFREY 权利人:RESEARCH CORP 摘要:In the synthesis of tetracyclines, a critical step is the stereospecific or stereoselective introduction of a hydroxyl group at the C-12(a) position, a novel method for the introduction of this critical hydroxy group is disclosed. Additionally, synthetic procedures for obtaining tetracycline precursors are discussed.
专利号:EP-0113566-A1 优先权日:1982-12-20 标题:New intermediate compounds for synthesis of aklavinones and their preparation 发明人:KISHI YOSHITO 权利人:MEIJI SEIKA KAISHA 摘要:A new compound of the formulan wherein R, is a hydrogen atom, a hydroxyl group or an alkoxyl group of 1-4 carbon atoms and R 2 is an alkyl group of 1-4 carbon atoms is now provided. This new compound is useful as intermediate for synthesis of aklavinones which may be coupled with sugars, for example, daunosamine to give anthracycline antibiotics. The new compound of this invention is produced by several reaction steps started from a 3-halo-5-substituted or unsubstituted naphthoquinone and a furan diene compound. This process involves new regiospecific Diels-Alder condensation and new asymmetric crossed aldol condensation.
专利号:US-2022378721-A1 优先权日:2019-10-24 标 题 :Protein kinase inhibitors and use thereof for treatment of neurodegenerative diseases 发明人:SRIDHAR JAYALAKSHMI; BRATTON MELYSSA; GOYAL NAVNEET; JHA VISHWAJEET; SCHROEDER RICHARD 权利人:XAVIER UNIV OF LOUISIANA 摘要:The present disclosure relates to compounds that act as protein kinase inhibitors, especially CK1δ and/or CK1ε inhibitors, which can be used to treat a serine threonine kinase-dependent disease and condition, such as neurodegenerative diseases like Alzheimer's Disease, and the synthesis of the same. Further, the present disclosure teaches the utilization of such compounds in a treatment for neurodegenerative diseases, including Alzheimer's disease.
专利号:US-11851651-B2 优先权日:2017-06-19 标 题 :Automated methods for scalable, parallelized enzymatic biopolymer synthesis and modification using microfluidic devices 发明人:BANAL JAMES; BERLEANT JOSEPH DON; SHEPHERD TYSON; BATHE MARK 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:Methods for the automated template-free synthesis of user-defined sequence controlled biopolymers using microfluidic devices are described. The methods facilitate simultaneous synthesis of up to thousands of uniquely addressed biopolymers from the controlled movement and combination of regents as fluid droplets using microfluidic and EWOD-based systems. In some forms, biopolymers including nucleic acids, peptides, carbohydrates, and lipids are synthesized from step-wise assembly of building blocks based on a user-defined sequence of droplet movements. In some forms, the methods synthesize uniquely addressed nucleic acids of up to 1,000 nucleotides in length. Methods for adding, removing and changing barcodes on biopolymers are also provided. Biopolymers synthesized according to the methods, and libraries and databases thereof are also described. Modified biopolymers, including chemically modified nucleotides and biopolymers conjugated to other molecules are described.
专利号:US-2023406804-A1 优先权日:2018-10-12 标题:Protein kinase inhibitors 发明人:SRIDHAR JAYALAKSHMI; JONES FRANK; STEVENS CHERYL 权利人:XAVIER UNIV OF LOUISIANA; THE ADMINISTRATORS OF THE TULANE EDUCATIONAL FUND 摘要:The present disclosure relates to compounds that act as protein kinase inhibitors, and the synthesis of the same. Further, the present disclosure teaches the utilization of such compounds in a treatment for proliferative diseases, including cancer, particularly breast cancer, and especially ER+ and/or HER2+ breast cancer.
专利号:US-5097051-A 优先权日:1989-02-10 标题 :Cyclic triketone compounds and trimethylsilyloxy butadiene compounds and their use in the preparation of daunomycinone derivatives 发明人:SCHEEREN JOHAN W; DEBIE JOANNES F M; DEVOS DIRK 权利人:PHARMACHEMIE BV 摘要:The invention provides novel cyclic triketone compounds of the formulae wherein S is H, alkyl or alkoxy and R* is a group of the formule wherein R<1> is methyl and R2 is an alkyl group containing at least 2 carbon atoms, or R<1> is an alkyl group having 1-4 carbon atoms and R<2> is an aryl group, a hetero aryl group, a -CH2OR min , a -CH2N @@ group, a -CH2SR sec group or a -CH2CH=CH2 group, wherein R min and R sec are alkyl groups having 1-4 carbon atoms. These compounds can be used for preparing daunomycinone and derivatives thereof. Daunomycinone is used for preparing daunomycin and adriamycin. By introducing chirality at C-1 of ring A in the preparation of said novel compounds by using a novel diene of formula (1) in a Diels-Alder reaction for said preparation, the chirality of C-3 is established in the subsequent reaction with LiC IDENTICAL CSi(CH3)3 in the synthesis of daunomycinone and derivatives thereof. This last reaction leads to the desired compound wherein OH at C-3 and OR at C-1 are in the cis-position with respect to each other.
参考标题:Asymmetric Synthesis Of Natural Cis-Dihydroarenediols Using Tetrahydroxynaphthalene Reductase And Its Biosynthetic Implications 作者:Nirmal Saha,Michael Müller,Syed Masood Husain |发布日期:2019.4.5 摘要:Asymmetric Reduction Of Hydroxynaphthoquinones To Secondary Metabolites, (3S,4R)-3,4,8- And (2S,4R)-2,4,8-Trihydroxy-1-Tetralone, A Putative Biosynthetic Diketo Intermediate And A Probable Natural Analogue, (3S,4R)-7-Acetyl-3,4,8-Trihydroxy-6-Methyl-3,4-Dihydronaphthalene-1(2H)-One, Using Nadph-Dependent Tetrahydroxynaphthalene Reductase (T4Hnr) Of Magnaporthe Grisea Is Described. This Work Implies
合成参考文献
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