CAS: 6723-30-4; O-(Tetrahydropyran-2-yl)-Hydroxylamine

相似化合物

694-54-2 6581-66-4 1233211-05-6

3,4-二氢-2H-吡喃置于对甲苯磺酸,一水合肼体系中,用 1,4-二氧六环,二氯甲烷,甲基叔丁基醚 作为反应溶剂,化学反应 4.0H,反应生成 O-(四氢-2H-吡喃-2-基)羟基胺
参考文献:New Hydroxamic Acid Derivatives Of Fluoroquinolones: Synthesis And Evaluation Of Antibacterial And Anticancer Properties
标题:New Hydroxamic Acid Derivatives Of Fluoroquinolones: Synthesis And Evaluation Of Antibacterial And Anticancer Properties
摘要:一系列新的氢氧酸衍生物(6A-F)在氟喹诺酮的c-3位置被设计和合成,采用多步合成方法.设计的概念是用氢氧酸替换氟喹诺酮中的3-羧酸,作为模拟酸的基团.本研究中的合成工作为基于纯氢氧酸的氟喹诺酮的合成提供了非常好示例.合成的化合物通过1H-NMR,电喷雾电离(esi)质谱和红外光谱进行表征.新化合物被测试其体外抗微生物和抗增殖活性.在六个衍生物中,化合物6E表现出中等的抗菌活性,能够抑制大肠杆菌和肺炎克雷伯菌的生长(最小抑菌浓度:4.00-8.00 µg/ml).化合物6B和6F对a549肺腺癌和hct-116结肠癌细胞系表现出非常好的生长抑制作用.
DOI:10.1248/cpb.C13-00797

专利信息

专利号:US-5817751-A
优先权日:1994-06-23
标 题 :Method for synthesis of diketopiperazine and diketomorpholine derivatives
发明人：SZARDENINGS ANNA KATRIN; CAMPBELL DAVID
权利人:AFFYMAX TECH NV
摘要:The present invention relates to the areas of organic and medicinal chemistry. More specifically, the present invention is concerned with combinatorial and solid phase methods for the synthesis of diverse diketopiperazine derivatives, and the use of such methods to create libraries of diverse diketopiperazine derivatives. The present invention has application in the areas of chemical synthesis, the screening for new diketopiperazine derivatives having beneficial medical properties and the use of such screening to provide compositions and methods including diketopiperazine derivatives for treating disease.

专利号:US-4987253-A
优先权日:1988-09-19
标 题 :Method for the synthesis of desferrioxamine B and analogs thereof
发明人：BERGERON RAYMOND J
权利人:UNIV FLORIDA
摘要:Disclosed is a synthesis of desferrioxamine B and analogs and homologs thereof beginning with the generation of the O-protected N-(4-cyanobutyl)hydroxylamine which is acylated at the O-benzylhydroxylamine nitrogen with either succinic or acetic anhydride. The resulting half-acid amide or amide respectively, is subjected to a series of high yield condensations and reductions which provide desferrioxamine B in 45% overall yield. Finally, a desamino analog of desferrioxamine is prepared in order to demonstrate the synthetic utility of the scheme as applied to desferrioxamine derivatives.

专利号:WO-9600391-A1
优先权日:1994-06-23
标题:Methods for the synthesis of diketopiperazines
发明人：CAMPBELL DAVID; GALLOP MARK A; GORDON ERIC M; LOOK GARY C; PATEL DINESH; SZARDENINGS ANNA KATRIN
权利人:AFFYMAX TECH NV; CAMPBELL DAVID; GALLOP MARK A; GORDON ERIC M; LOOK GARY C; PATEL DINESH; SZARDENINGS ANNA KATRIN
摘要:Libraries of diverse diketopiperazines bound to a support and methods for synthesizing diketopiperazines on a solid support are described. These libraries have utility in the area of drug design as they can be screened against biological substances to identify compounds which have desirable biological activity.

专利号:US-6281245-B1
优先权日:1996-10-28
标 题:Methods for solid-phase synthesis of hydroxylamine compounds and derivatives, and combinatorial libraries thereof
发明人：PATEL DINESH V; NGU KHEHYONG
权利人:VERSICOR INC
摘要:A novel method for generating hydroxylamine, hydroxamic acid, hydroxyurea, and hydroxylsulfonamide compounds is disclosed. The method involves the nucleophilic attack of an alkoxyamine on a suitable solid phase support. Techniques of combinatorial chemistry can then be applied to the immobilized alkoxyamine to generate a diverse set of compounds. Cleavage of the compounds from the support yields a library of hydroxylamine or hydroxylamine derivative compounds, which can be screened for biological activity (e.g., inhibition of metalloproteinases).

专利号:US-6541276-B2
优先权日:1996-10-28
标题:Methods for solid-phase synthesis of hydroxylamine compounds and derivatives and combinatorial libraries thereof
发明人：PATEL DINESH V; NGU KHEHYONG
权利人:VERSICOR INC
摘要:A novel method for generating hydroxylamine, hydroxamic acid, hydroxyurea, and hydroxylsulfonamide compounds is disclosed. The method involves the nucleophilic attack of an alkoxyamine on a suitable solid phase support. Techniques of combinatorial chemistry can then be applied to the immobilized alkoxyamine to generate a diverse set of compounds. Cleavage of the compounds from the support yields a library of hydroxylamine or hydroxylamine derivative compounds, which can be screened for biological activity (e.g., inhibition of metalloproteases).

专利号:US-6989401-B2
优先权日:2000-07-19
标题:Sulfonic acid derivatives of hydroxamic acids and their use as medicinal products
发明人：MAEDA KAZUHIRO; SONDA SHUJI; TAKEMOTO TADAHIRO; GOTO TOMOKAZU; KOBAYASHI FUJIO; KAJII MASAHIKO; KOMORITA NARUYASU; HIRAYAMA FUMIHIRO
权利人:MITSUBISHI PHARMA CORP
摘要:The present invention relates to a novel sulfonic acid derivative of hydroxamic acid or a pharmacologically acceptable salt thereof. More particularly, the present invention relates to a sulfonic acid derivative of hydroxamic acid or a pharmacologically acceptable salt thereof, which is useful as an inhibitor of lipopolysaccharides (LPS). In addition, the present invention relates to a novel intermediate compound useful for the synthesis of this sulfonic acid derivative of hydroxamic acid.