CAS: 244-63-3; 9H-Pyrido[3,4-B]Indole

相似化合物

486-84-0 83911-48-2 18203-06-0

上下游产品

tetrahydrobetacarboline harmane 1,2,3,4-tetrahydro-β-carboline-3-carboxylic acid indole9-benzyl-9H-pyrido3,4-bindole H-β-carbolinium; dibromide2-(3-trimethylammonio-propyl)-9H-β-carbolinium; dibromide phenyl(9H-pyrido[3,4-b]indol-9-yl)methanone indole9-benzyl-9H-pyrido3,4-bindole 9-methylnorharmane

L-色氨酸置于potassium Dichromate,水,溶剂黄146,Sodium Hydroxide体系中,化学反应生成9H-吡啶[3,4-B]吲哚
参考文献:新型n 9-异二价β-咔啉类化合物作为血管生成抑制剂的合成及生物学评价
标题:新型n 9-异二价β-咔啉类化合物作为血管生成抑制剂的合成及生物学评价
摘要:抽象的 已经合成了一系列新颖的n 9-杂二价β-咔啉.测试了所有这些新化合物对六种肿瘤细胞的体外抗癌活性.在这些分子中,化合物5B和5W表现出强大的细胞毒性活性,Ic 50值低于20μm.还评估了所选化合物在小鼠中的急性毒性和抗肿瘤功效,化合物5B和5W在肉瘤180和lewis肺癌动物模型中显示出超过40%的肿瘤抑制率.初步的结构-活性关系(sar)分析表明:(1)c 1-甲基化和c 7-甲氧基化有助于增加活性;(2)在β-咔啉核心的位置1上的3-吡啶基或2-噻吩基取代基,以及在另一个β-咔啉环上的芳基取代基可能对这类化合物的细胞毒性作用有害.对初步作用机理的研究表明,化合物5B在鸡绒膜尿囊膜(cam)分析中具有明显的血管生成抑制作用.
Doi:10.1080/14756366.2018.1497619

专利信息

专利号:US-8822702-B2
优先权日:2002-12-20
标 题 :Synthesis of amines and intermediates for the synthesis thereof
发明人：BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL
权利人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL; BASF SE
摘要:The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, n nor especially of amides of the formula II,n n nwherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.

专利号:US-9353057-B2
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
发明人：GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
权利人:XENOPORT INC
摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

专利号:US-2011245503-A1
优先权日:2008-11-28
标题 :Enantioselective synthesis of asymmetric beta-carboline intermediates
发明人：SANTOS LEONARDO; ESPINOZA MORAGA MARLENE; SHANKARAJAH NAGULA
权利人:UNIV TALCA
摘要:Described herein is a new asymmetric synthesis of imines to obtain β-carboline derivatives useful as key intermediate compounds for the synthesis of phosphodiesterase inhibitors using a new process with palladium or ruthenium hydride and/or nickel boride to reduce chiral intermediates. The use of chloroformate chiral auxiliaries is further described for the reduction and asymmetric hydrogenation of imines to obtain β-carboline derivatives and intermediate compounds used in the preparation thereof.

专利号:US-6849743-B2
优先权日:1997-08-15
标 题 :Synthesis of clasto-lactacystin β-lactone and analogs thereof
发明人：SOUCY FRANCOIS; FLAMONDON LOUIS; BEHNKE MARK; ROUSH WILLIAM
权利人:MILLENNIUM PHARM INC
摘要:The present invention is directed to an improved synthesis of clasto-lactacystin-β-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin-β-lactones, and analogs thereof and their use as proteasome inhibitors.

专利号:US-6528646-B2
优先权日:1998-01-30
标题 :Intermediates for the synthesis of debromohymenialdisine and process thereof
发明人：HORNE DAVID A; YAKUSHIJIN KENICHI
权利人:UNIV COLUMBIA
摘要:The synthesis of C 11 N 5 marine sponge alkaloids (±)-hymenin (1), stevensine (2), hymenialdisine (3), and debromohymenialdisine (4) is described. These natural products are the primary family members of the sponge metabolites that contain a fused pyrrolo[2,3-c]lazepin-8-one ring system with either a 2-aminoimidazole (AI) or glycocyamidine appendage. The key steps in the synthesis centered around the generation of novel azafulvenium ions and their regioselective heterodimerization with AI in order to create the tricyclic core. A rarely used protodebromination/oxidation strategy was employed to selectively generate the desired a-bromo substitution pattern seen in hymenialdisine (3). In addition, the AI moiety was shown to be a useful precursor to the glycocyamidine unit found in 3 and 4, which suggests that AI derived natural products may be the biogenic forerunners to glycocyamidine metabolites.

专利号:US-9085538-B2
优先权日:2010-07-26
标题:Process for the preparation of key intermediates for the synthesis of statins or pharmaceutically acceptable salts thereof
发明人：CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO
权利人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO; LEK PHARMACEUTICALS
摘要:The invention relates to commercially viable process for the synthesis of key intermediates for the preparation of statins, in particular Rosuvastatin and Pitavastatin or respective pharmaceutically acceptable salts thereof. A new simple and short synthetic route for key intermediates is presented which benefits from the use of cheap and readily available starting materials, by which the conventionally most frequently used DIBAL-H as reducing agent can be avoided.