CAS: 172732-68-2; 2-((3-(2-Amino-2-Oxoacetyl)-1-Benzyl-2-Ethyl-1H-Indol-4-yl)Oxy)Acetic Acid

上下游产品

[[3-(2-amino-1,2-dioxoethyl)-2-ethyl-1-(phenylmethyl)-1H-indol-4-yl]oxy]acetic acid methyl ester tert-butyl 2-(3-(2-amino-2-oxoacetyl)-1-benzyl-2-ethyl-1H-indol-4-yloxy)acetate 3-chloro-2-iodophenyl N,N-dimethyl O-carbamate tert-butyl 2-(1-benzyl-2-ethyl-1H-indol-4-yloxy)acetate

📜3-氯-2-碘苯酚置于bis-Triphenylphosphine-Palladium(II) Chloride,Palladium Diacetate Potassium Tert-Butylate,四丁基氟化铵,三溴化硼,Sodium Hydride,Potassium Carbonate,三氟乙酸,1,3-双(2,6-二异丙基苯基)氯化咪唑鎓体系中,用 二氯甲烷,N,N-二甲基甲酰胺,甲苯,乙腈 用作溶剂,化学反应 23.0H,反应生成伐瑞拉迪
参考文献:由2,3-二卤代苯酚选择性合成4-和7-烷氧基吲哚:在制备磷脂酶a 2吲哚抑制剂中的应用
标题:由2,3-二卤代苯酚选择性合成4-和7-烷氧基吲哚:在制备磷脂酶a 2吲哚抑制剂中的应用
摘要:已经从市售的起始原料例如3-卤代苯酚和3-氯苯甲醚开发了4-和7-烷氧基吲哚的有效和区域选择性合成.定向原位金属化,然后进行两个钯催化的过程,Sonogashira偶联和串联胺化/环化反应,可以合成区域化学上纯的4和7取代的吲哚.该策略已成功地用于制备已知的2-[3-(2-氨基-2-氧代乙酰基)-1-苄基-2-乙基-1 H-吲哚-4-基氧基]乙酸(ly315920)磷脂酶a 2的抑制剂.
Doi:10.1021/jo070643Y

专利信息

专利号:US-12098115-B2
优先权日:2016-09-15
标 题:Methods and compositions for terpenoid synthesis
发明人：GRENNING ALEXANDER JAMES
权利人:UNIV FLORIDA
摘要:In one aspect, the disclosure relates to methods for preparation of terpene and terpene-like molecules. In a further aspect, the disclosure relates to the products of the disclosed methods, i.e., terpene and terpene-like molecules prepared using the disclosed methods. Intermediates for the synthesis of a wide variety of terpenoids are γ-allyl Knoevenagel adducts or quasi γ-allyl Knoevenagel adducts are disclosed. In various aspects, methods of preparing terpenoids through these intermediates are disclosed. The methods can comprise α-alkylation of an allylic electrophile followed by ring-closure metathesis to a polycyclic terpenoid structure. In a further aspect, the disclosure pertains to terpenoid frameworks, and compounds prepared via disclosed oxidation and substitution reactions on the disclosed terpenoid frameworks. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

专利号:US-8269047-B2
优先权日:2009-07-23
标题 :Synthesis of alpha-halo enones and enals
发明人：ZHANG LIMING; YE LONGWU
权利人:ZHANG LIMING; YE LONGWU; UNIV NEVADA
摘要:A method for preparing an α-halo enal or enone from an unprotected propargyl alcohol and an electrophilic halogen source catalyzed by the combination of a gold catalyst complex and a metal co-catalyst complex is disclosed. The method can be further enhanced by addition of an additive that facilitates suppression of a des-halo derivative.

专利号:US-7579433-B2
优先权日:2003-04-30
标题:Methods and compositions for treatment of arthritis and cancer
发明人：GOPALAKRISHNAKONE PONNAMPALAM; THWIN MAUNG-MAUNG; SATO KAZUKI
权利人:UNIV SINGAPORE
摘要:The present invention provides a new 18-residue homodimerized peptide, designated PIP [59-67] dimer (SEQ ID NO: 1), which is a mutant of the optimized anti-inflammatory peptide P-NT.II, the patent for which has recently been filed [1]. P-NT.II has the potential to modulate both the inflammatory and bone damaging components of rheumatoid arthritis, and was originally designed on the basis of the primary structure of the anti-inflammatory protein termed ‘Phospholipase Inhibitor from Python (PIP)’ [2]. Using solid phase chemistry, variants of P-NT.II were designed and examined for inhibitory activity against secretory phospholipase A2 (sPLA2), a key enzyme involved in the inflammatory pathway, and matrix metalloproteinases (MMPs) that are involved in the remodeling and degradation of the extracellular matrix in rheumatoid arthritis (RA) and cancer. Among the family of mutants tested, the dimerized peptide was found to be the most potent inhibitor against sPLA2 as well as the human recombinant MMP-1. This invention provides the utility of the peptide analogue PIP [59-67] dimer as a potential therapeutic agent for modulation of inflammatory diseases such as rheumatoid arthritis, and cancer. This invention relates to all the polypeptide analogues (SEQ ID NO: 1 to 3) and polynucleotides (SEQ ID NO: 4), and to the use of those polypeptides and polynucleotides, their synthetic chemical analogues or variants that inhibit activity and synthesis of sPLA2 and MMPs, in the diagnosis, study, prevention and treatment of rheumatoid arthritis and/or cancer.

专利号:WO-0144184-A1
优先权日:1999-12-16
标题:Synthesis of indole-containing spla2 inhibitors
发明人：MARTINELLI MICHAEL JOHN; SAWYER JASON SCOTT
权利人:LILLY CO ELI; MARTINELLI MICHAEL JOHN; SAWYER JASON SCOTT
摘要:A method of making a compound include reacting a compound represented by formula (I), with a base, to form the compound of formula (II); and where R1 is H, R10 or -C(O)R10; R2 is R20 -OR20, -SR20, -NR20R20' or -C(O)R20;R3, R4, R5, R6 and R7 are each individually H, halogen, R, -OR, -SR, -NRR', -C(O)R, -C(O)OR, -S(O)R or -S(O)2R; provided that at least one of R4 and R5 is not H; each R, R10 and R20 is individually alkyl, alkenyl, alkynyl, aryl or heterocyclic radical; each R' and R20' is individually H, alkyl, alkenyl, alkynyl, aryl or heterocyclic radical; and W is a trisubstituted phosphorous. The method provides an alternative route to indole-3-glyoxylamide compounds.

专利号:US-9422321-B2
优先权日:2010-09-07
标题 :Pyrimidine nucleoside derivatives, synthesis methods and uses thereof for preparing anti-tumor and anti-virus medicaments
发明人：CHANG JUNBIAO; AN HAOYUN; YU XUEJUN; GUO XIAOHE
权利人:CHANG JUNBIAO; AN HAOYUN; YU XUEJUN; GUO XIAOHE; HIGH & NEW TECH RES CENTER HENAN ACAD OF SCIENCES; ZHENGZHOU GRANLEN PHARMATECH LTD; UNIV ZHENGZHOU
摘要:The present invention relates to the field of pharmacochemistry. Disclosed are fluorinated and azido-substituted pyrimidine nucleoside derivatives, particularly compounds of the formula shown below: n nAlso disclosed are methods of preparation and uses for these compounds. The compounds can be used for preparing medicaments for treating diseases such as tumors and viral infections, and can be used separately or in combination with other medicaments. The compounds also have effective activity against diseases such as tumors and viral infections, while having few side effects, and thus have potential application value.

专利号:WO-0144185-A1
优先权日:1999-12-16
标题 :Carbon monoxide-based synthesis of spla2 inhibitors
发明人：SAWYER JASON SCOTT
权利人:LILLY CO ELI; SAWYER JASON SCOTT
摘要:A method of making a compound, comprises reacting a compound represented by formula (I), with CO and a catalyst, to form the compound of formula (II); where formula (I) is and, formula (II) is and where R2 is selected from the group consisting of R20 -OR20, -SR20, -NR20R20'and -C(O)R20; R3, R4, R5, R6 and R7 are each individually selected from the group consisting of H, halogen, R, -OR, -SR, -NRR', -C(O)R, -C(O)OR, -S(O)R and -S(O)2R; provided that at least one of R4 and R5 is not H; each R and R20 is individually selected from the group consisting of alkyl, alkenyl, alkynyl, aryl and heterocyclic radical; and each R' and R20' is individually selected from the group consisting of H, alkyl, alkenyl, alkynyl, aryl and heterocyclic radical. The method provides an alternative route to indole-3-glyoxylamide compounds.