CAS: 630420-16-5; Tert-Butyl ((S)-1-((2S,4R)-4-((7-Chloro-4-Methoxyisoquinolin-1-yl)Oxy)-2-(((1R,2S)-1-((Cyclopropylsulfonyl)Carbamoyl)-2-Vinylcyclopropyl)Carbamoyl)Pyrrolidin-1-yl)-3,3-Dimethyl-1-Oxobutan-2-yl)Carbamate

上下游产品

CAS号1028252-93-8 (2S,4R)-4-(7-ch... | CAS号62965-35-9 N-B°C-L-叔亮氨酸 | CAS号1028252-17-6 (2S,4R)-tert-bu... | CAS号953421-74-4 4-溴-1,7-二氯异喹啉 | CAS号630423-36-8 1,7-二氯-4-甲氧基异喹啉 | CAS号1615-02-7 4-氯肉桂酸 | CAS号24188-74-7 7-氯异喹啉-1(2H)-酮 | CAS号1028252-13-2 4-溴-7-氯异喹啉-1(2H)-酮

1,7-Dichloroisoquinolin-4-Ol置于potassium Tert-Butylate,N,N-二异丙基乙胺,N-[(Dimethylamino)-3-Oxo-1H-1,2,3-Triazolo[4,5-B]Pyridin-1-Yl-Methylene]-N-Methylmethanaminium Hexafluorophosphate,三甲基硅烷化重氮甲烷体系中,用 正己烷,二氯甲烷,二甲基亚砜,乙腈 作为反应溶剂,化学反应 49.5H,反应生成 Asunaprevir; (1R,2S)-N-[(1,1-二甲基乙氧基)羰基]-3-甲基-L-缬氨酰-(4R)-4-[(7-氯-4-甲氧基-1-异喹啉基)氧基]-L-脯氨酰-1-氨基-N-(环丙基磺酰基)-2-乙烯基环丙基甲酰胺
参考文献:口服有效的ns3蛋白酶抑制剂asunaprevir(bms-650032)的发现,可用于治疗丙型肝炎病毒感染
标题:口服有效的ns3蛋白酶抑制剂asunaprevir(bms-650032)的发现,可用于治疗丙型肝炎病毒感染
摘要:Asunaprevir的发现(bms-650032,24)进行说明.ns3 / 4A酶的这种三肽酰基磺酰胺抑制剂目前正在治疗丙型肝炎病毒感染的iii期临床试验中.通过采用离体兔心脏模型筛选心血管(cv)负债(hr和snrt的变化)来发现24种,这些负债是导致该化学系列bms-605339中较早的铅停用的原因(1),来自临床试验.与cv效应有关的结构-活性关系(sar)确定了分子p2 *亚位点的微小结构变化对给定化合物的cv谱具有重大影响.在大鼠和狗中的抗病毒活性,临床前pk谱和毒理学研究支持bms-650032的临床开发(24).
DOI:10.1021/jm500297K

专利信息

专利号:US-11866398-B2
优先权日:2018-05-15
标 题:Total synthesis of prostaglandin J natural products by stereoretentive metathesis
发明人：LI JIAMING; CHEN XU; AHMED TONIA S; STOLTZ BRIAN M; GRUBBS ROBERT H
权利人:CALIFORNIA INST OF TECHN
摘要:This invention relates generally to the synthesis of Δ12-Prostaglandin J product using stereoretentive ruthenium olefin metathesis catalysts supported by dithiolate ligands. Δ12-Prostaglandin J products were generated with excellent selectivity (>99% Z) and in moderate to high/good yields (47% to 80% yield; 58% to 80% yield).

专利号:US-8193384-B2
优先权日:2005-07-29
标 题 :Polymer-bound phosphitylating reagents for the synthesis of organophosphorus compounds
发明人：PARANG KEYKAVOUS; AHAMDIBENI YOUSEF
权利人:PARANG KEYKAVOUS; AHAMDIBENI YOUSEF; RHODE ISLAND EDUCATION
摘要:The synthesis and biochemical utility of modified oligonucleotides containing diphosphodiester internucleotide linkages. The synthesis of these compounds was carried out using diphosphitylating reagents. Oligonucleotides containing diphosphate diester bridges wherein said oligonucleotides are synthesized via a solid-phase synthesis strategy to form modified oligonucleotides. Diphosphitylating, triphosphitylating, tetraphosphitylating, β-triphosphitylating, bifunctional diphosphitylating, bifunctional triphosphitylating, and bifunctional tetraphosphitylating reagents wherein, the phosphorus atoms are linked together through oxygen, sulfur, amino, or methylene groups and/or are substituted with chlorine, diisopropylamine and cyanoethoxy groups.

专利号:US-2010143980-A1
优先权日:2007-02-22
标题:Synthesis of novel xylosides and potential uses thereof
发明人：BALAGURUNATHAN KUBERAN; MANIVANNAN ETHIRAJAN; XYLOPHONE V VICTOR; TRAN VY MY; NGUYEN KHIEM
权利人:BALAGURUNATHAN KUBERAN; MANIVANNAN ETHIRAJAN; XYLOPHONE V VICTOR; TRAN VY MY; NGUYEN KHIEM
摘要:The present invention includes a xyloside for use in inducing synthesis of a glycosaminoglycan in a cell, the xyloside having a chemical structure of one of Formula (1), Formula (2), Formula (3), Formula (4), Formula (5), Formula (6), Formula (7), Formula (8), Formula (9), or Formula (10) as shown herein. Also, the present invention includes a method of making a xyloside for use in inducing synthesis of a glycosaminoglycan in a cell, wherein the method is performed with “Clickâ€? chemistry. Additionally, the present invention includes a method of administering a xyloside so as to induce synthesis of a glycosaminoglycan in a cell.

专利号:US-10751419-B2
优先权日:2014-05-01
标题:Method for synthesis of reactive conjugate clusters
发明人：MIGAWA MICHAEL T; YU JINGHUA; WAN W BRAD; PATEL SAYTEN P; VASQUEZ GUILLERMO; KINBERGER GARTH A; PRAKASH THAZHA P; SETH PUNIT P; SWAYZE ERIC E
权利人:IONIS PHARMACEUTICALS INC
摘要:Provided herein are improved methods for the synthesis of reactive conjugate clusters and intermediates used in such methods. In particular, improvements are provided that enhance the synthesis of reactive conjugate clusters by reducing the number of synthetic steps required. The reactive conjugate clusters prepared using the improved methods don't include any transacylation impurities that are formed using existing methods. The improved methods also provide an increase in overall yield and a cost benefit over existing methods.

专利号:US-5139940-A
优先权日:1989-10-26
标题 :Activation compounds and methods of synthesis of activation compounds
发明人：ISAACS STEPHEN T; CIMINO GEORGE D; METCHETTE KENNETH C; TESSMAN JOHN W
权利人:ISAACS STEPHEN T; CIMINO GOERGE D; METCHETTE KENNETH C; TESSMAN JOHN W
摘要:The invention is directed to isopsoralen compound compositions that contain a variety of substitutions which yet permit their binding to nucleic acid polymers. Reaction conditions that activate these bound isopsoralens results in covalent crosslinking to the nucleic acid polymers. The resultant complex is inhibited from being a template for the template-directed enzymatic synthesis of a complementary nucleic acid polymer. Beside the isopsoralens compositions, the invention includes their synthesis, the nucleic acid complex production and detection, and the above inhibitory method of use of the isopsoralens.

专利号:US-10011580-B2
优先权日:2016-04-21
标题:Diastereoselective synthesis of (±)-epianastrephin, (±)-anastrephin and analogs thereof
发明人：WALSE SPENCER S; KUZMICH DANIEL
权利人:US AGRICULTURE
摘要:A process for the synthesis of trans-fused γ-lactones having Formula (IV) from substituted cyclic ketones having Formula (I). A diastereoselective synthesis of (±)-epianastrephin (1) (wherein: R 1 is ethenyl, R 2 and R 3 is methyl, and n is 1), (±)-anastrephin (2) (wherein: R 2 is ethenyl, R 1 and R 3 is methyl and n is 1), and analogs thereof (wherein: R 1 is H, C 1-5 alkyl, C 2-6 alkenyl or C 2-6 alkynyl, R 2 is H, C 1-5 alkyl, C 2-6 alkenyl or C 2-6 alkynyl, R 1 and R 2 together with the carbon atom they are attached form a C 3-6 cycloalkyl ring, R 3 is C 1-5 alkyl and n is 0-2):