CAS: 1576-35-8; 4-Methylbenzenesulphonylhydrazide

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CAS号98-59-9 对甲苯磺酰氯(PTSC) | CAS号1666-17-7 苯甲醛对甲苯磺酰腙 | CAS号7803-57-8 水合肼 | CAS号64-17-5 乙醇 | CAS号110576-17-5 N-[(E)-indeno[2... | CAS号106368-34-7 5-Amino-1-[(4-m... | CAS号105577-48-8 N'-(5,5-dimethy... | CAS号109333-73-5 对甲苯磺酰肼-D3 | CAS号31378-03-7 2-(对甲苯磺酰基)苯乙酮 | CAS号71899-75-7 2-hydroxy-2-phe... | CAS号4545-21-5 苯乙酮对甲苯磺酰腙 | CAS号4545-20-4 二苯甲酮对家苯磺酰腙 | CAS号14661-69-9 4-甲基-2-(2-氯代-2-...

对甲苯磺酸甲酯置于一水合肼体系中,用 甲醇 用作溶剂,化学反应生成对甲苯磺酰肼
参考文献:基于结构的新型己糖激酶2抑制剂的发现.
标题:基于结构的新型己糖激酶2抑制剂的发现.
摘要:Hexokinase 2(hk2)在大多数人类癌症中均过表达,并且已被证明是癌症治疗的有希望的靶标.在这项研究中,基于hk2的结构,我们筛选了超过600万种化合物以获得铅.然后设计,合成总共26种(e)-N'-(2,3,4-三羟基亚苄基)芳基酰肼衍生物,并评估其针对两种癌细胞系的hk2酶活性和ic50值.26种目标化合物中的大多数都具有出色的体外活性.其中,化合物3J对hk2酶活性的抑制作用最强,Ic50为0.53+/-0.13μm,对sw480细胞的生长抑制作用最强,Ic50为7.13+/-1.12μm,值得进一步研究.
Doi:10.1016/j.Bioorg.2020.103609

专利信息

专利号:US-9783549-B2
优先权日:2013-11-04
标题:Macrocyclization reactions and intermediates useful in the synthesis of analogs of halichondrin B
发明人：FANG FRANCIS G; KIM DAE-SHIK; CHOI HYEONG-WOOK; CHASE CHARLES E; LEE JAEMOON
权利人:EISAI R&D MAN CO LTD
摘要:The invention provides methods for the synthesis of eribulin or a pharmaceutically acceptable salt thereof (e.g., eribulin mesylate) through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Homer-Wadsworth-Emmons olefination), Dieckmann reaction, catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic intermediate. The invention also provides compounds useful as intermediates in the synthesis of eribulin or a pharmaceutically acceptable salt thereof and methods for preparing the same.

专利号:US-9676707-B2
优先权日:2015-02-18
标题 :Process for the synthesis of [6,6]-phenyl-C61butyric acid pentyl ester (PC61BP)
发明人：KUMAR RACHANA; NAQVI Samya; GUPTA NEHA; CHAND SURESH
权利人:COUNCIL SCIENT IND RES
摘要:A total green, eco-friendly process for the synthesis of new acceptor molecule [6,6]-phenyl-C 61 -butyric acid pentyl ester (PC61BP) in high yields is carried under aerobic conditions showing better performance as acceptor in organic solar cells. More importantly this process causes the low cost synthesis of PC61BP in good yield without involving harmful and costly catalysts or chemicals.

专利号:US-11613514-B2
优先权日:2016-03-25
标题:Crystal forms and methods of synthesis of (2R, 6R)-hydroxynorketamine and (2S, 6S)-hydroxynorketamine
发明人：THOMAS CRAIG; ZARATE CARLOS; MOADDEL RUIN; GOULD TODD; ZANOS PANOS; MORRIS PATRICK
权利人:US HEALTH; UNIV MARYLAND
摘要:The disclosure provides a method for synthesizing free base forms of (2R,6R)-hydroxynorketamine (HNK) and (2S,6S)-hydroxynorketamine. In an embodiment synthesis of (2R,6R)-hydroxynorketamine (HNK) includes preparation of (R)-norketamine via chiral resolution from racemic norketamine via a chiral resolution with L-pyroglutamic acid. The disclosure also provided crystal forms of the corresponding (2R,6R)-hydroxynorketamine (HNK) and (2S,6S)-hydroxynorketamine hydrochloride salts.

专利号:US-8779207-B2
优先权日:2012-08-31
标题 :Method for synthesis of [6,6]-phenyl-C61-butyric acid methyl ester (PCBM) and fullerene derivatives
发明人：NG KA MING; ZHUANG JIANLE; TSENG NAI WEN; YU YONG
权利人:NG KA MING; ZHUANG JIANLE; TSENG NAI WEN; YU YONG; NANO & ADVANCED MATERIALS INST LTD
摘要:The present subject matter relates to methods for the synthesis of [6,6]-phenyl-C 61 -butyric acid methyl ester (PCBM) and fullerene derivatives in a yield of at least 40%.

专利号:US-4239689-A
优先权日:1978-12-18
标题 :Total synthesis of the utero-evacuant substance d,l-zoapatanol
发明人：KANE VINAYAK V
权利人:ORTHO PHARMA CORP
摘要:A method for the synthesis of racemic 2S*, 3R*-6E-(2'-hydroxyethylidene)-2-methyl-2-(4',8'-dimethyl-5'-oxo-7'-nonenyl)-oxepan-3-ol is described. The naturally occurring product, 2S, 3R-6E-(2'-hydroxyethylidene)-2-methyl-2-(4',8'-dimethyl-5'-oxo-7'-nonenyl)-oxepan-3-ol, is one of the active components of the zoapatle plant.

专利号:US-7691635-B2
优先权日:2004-03-26
标题 :Labeling reagents, methods for the synthesis of such reagents and methods for the detection of biological molecules
发明人：LAAYOUN ALI; BERNAL-MENDEZ ELOY
权利人:BIOMERIEUX SA
摘要:The present invention relates to a temperature-stable labeling reagent of formula (0): n nin which:n R 1 represents H or an alkyl, aryl or substituted aryl group, R 2 represents a detectable marker or at least two detectable markers interlinked by at least one multimeric structure, L is a linker arm comprising a linear chain of at least two covalent bonds and n is an integer equal to 0 or 1, R 3 and R 4 represent, independently of one another: H, NO 2 , Cl, Br, F, I, R 2 -(L) n -Y—X—, OR, SR, NR 2 , R, NHCOR, CONHR, COOR, —CO—NH—(CH 2 ) 3 —(O—CH 2 —CH 2 ) 3 —CH 2 —NH—R 2 , —CO—NH—(CH 2 ) 3 —(O—CH 2 —CH 2 ) 4 —CH 2 —NH—R 2 with R=alkyl or aryl, A is a linker arm comprising at least one covalent double bond enabling the conjugation of the diazo function with the aromatic ring and u is an integer between 0 and 2, preferably 0 or 1, —Y—X— represents —CONH—, —NHCO—, —CH 2 O—, —CH 2 S—, —Z— represents —NH—, —NHCO—, —CONH— or —O—, m is an integer between 1 and 10, preferably between 1 and 3, and p is an integer between 1 and 10, preferably between 1 and 3. n The present invention also describes a method for the synthesis of said labels and also applications for the labeling of biological molecules, in particular of nucleic acids, with a labeling reagent bearing the diazomethyl function. n The invention is particularly suitable for use in the field of diagnostics.