CAS: 555-96-4; Benzylhydrazine

上下游产品

benzaldehyde, hydrazone benzaldehyde benzyl chloride N,N-dibenzylhydrazine3-benzyl-carbazic acid-(2-hydroxy-ethyl ester) is°Carboxazid 2-benzyl-2,3-dihydrophthalazine-1,4-dione 2-benzyl-5-methyl-1,2-dihydro-pyrazol-3-one

苯甲醛腙置于k12(Ga4(1,5-Bis(2,3-Dihydroxybenzamido)Naphthalene))6,Potassium Phosphate,吡啶硼烷体系中,用 重水 作为反应溶剂,化学反应 22.0H,以34%的收率获得产物苄基肼
参考文献:由超分子宿主和吡啶-硼烷辅因子催化的化学选择性和位点选择性还原
标题:由超分子宿主和吡啶-硼烷辅因子催化的化学选择性和位点选择性还原
摘要:超分子催化剂模仿酶的机制,在温和和水性条件下实现大的速率加速和精确的选择性.虽然在超分子宿主促进的小分子合成方面取得了重大进展,但这种反应性在复杂生物分子的化学选择性和位点选择性修饰中的应用实际上仍未得到探索.我们在这里报告了一种超分子系统,其中吡啶-硼烷与各种分子(包括烯酮,酮,醛,肟,腙和亚胺)的共包封在碱性水条件下有效减少.在将未受保护的赖氨酸置于宿主介导的还原胺化条件下后,我们观测到了出色的 ε 选择性,表明在不牺牲反应性的情况下,同一分子内的不同客体结合是可能的.受酶系统对复杂生物分子的翻译后修饰的启发,我们随后将这种超分子反应应用于 11 个氨基酸肽链和人胰岛素中单个赖氨酸残基的位点选择性标记.
DOI:10.1021/jacs.0C12479

专利信息

专利号:US-7414106-B2
优先权日:2003-06-19
标 题 :Synthesis of peptide α-thioesters
发明人：CAMARERO JULIO A; MITCHELL ALEXANDER R; DE YOREO JAMES J
权利人:L LIVERMORE NAT SECURITY LLC
摘要:Disclosed herein is a new method for the solid phase peptide synthesis (SPPS) of C-terminal peptide α thioesters using Fmoc/t-Bu chemistry. This method is based on the use of an aryl hydrazine linker, which is totally stable to conditions required for Fmoc-SPPS. When the peptide synthesis has been completed, activation of the linker is achieved by mild oxidation. The oxidation step converts the acyl-hydrazine group into a highly reactive acyl-diazene intermediate which reacts with an α-amino acid alkylthioester (H-AA-SR) to yield the corresponding peptide α-thioester in good yield. A variety of peptide thioesters, cyclic peptides and a fully functional Src homology 3 (SH3) protein domain have been successfully prepared.

专利号:US-2004053355-A1
优先权日:2000-05-26
标题:Modular approach to on-line synthesis, drug discovery and biochemical transformations using immobilized enzyme reactors
发明人：WAINER IRVING; MARKOGLOU NEKTARIA
摘要:A coupled system using extremely different enzymes with incompatible cofactors and reaction conditions has been constructed using standard liquid chromatographic formats and open tubular formats. One of the significant aspects of the present invention lies in the development of the liquid chromatographic on-line enzyme cascade. This has been illustrated by the biosynthetic pathway involving dopamine beta-hydroxylase and phenylethanolamine N-methyltransferase which encompass the synthesis of the key neurotransmitters, norepinephrine and epinephrine. The results demonstrate for the first time the immobilization of dopamine beta-hydroxylase and phenylethanolamine N-methyltransferase. The IMERs are active and can be used in a liquid chromatographic format for qualitative and quantitative determinations. The IMER-HPLC system can be used to carry out standard Michaelis-Menten enzyme kinetic studies and to quantitatively determine enzyme kinetic constants, identify specific enzyme inhibitors, provide information regarding the mode of inhibition and the inhibitor constants (K i ). A second significant aspect of the present invention lies in the ability of the immobilized enzyme reactors to be used independently or as a combination, thus providing a unique opportunity to explore the interrelationships between these enzymes, to investigate the source of diseases and to design new drug entities for identified clinical syndromes.

专利号:US-3978140-A
优先权日:1974-09-23
标题 :Process for the preparation of carbinols
发明人：LANE CLINTON FISHER; MYATT HAL LESLIE
权利人:ALDRICH BORANES INC
摘要:Organic compounds containing a carboxylic acid or carboxylic acid anhydride group are reduced when contacted with an alkali metal borohydride and a boron trihalide in a liquid medium in which diborane is soluble in the form of a labile borane adduct. Hydrolysis of the reaction mixture then provides a useful synthesis of the corresponding carbinols. n The alkali metal borohydride-boron trihalide reagent may either be preformed and reacted subsequently with an organic compound containing a carboxylic acid or anhydride group, or the alkali metal borohydride-boron trihalide reagent may be produced in the presence of an organic compound containing a carboxylic acid or anhydride group. This development makes it possible to synthesize a wide variety of carbinols which are valuable and useful intermediates in organic synthesis.

专利号:US-6867202-B1
优先权日:1997-06-25
标 题 :Treatment of insulin resistance
发明人：CARPINO PHILIP ALBERT; CHIU CHARLES KWOK-FUNG; PAN LYDIA CODETTA; LEFKER BRUCE ALLEN; TREADWAY JUDITH LEE; ZAWISTOSKI MICHAEL PAUL
权利人:PFIZER
摘要:This invention is directed to methods of treating insulin resistance in a mammal which comprise administering an effective amount of a compound of formula I, n n nwhere the variables are defined in the specification, or the stereoisomeric mixtures, diastereomerically enriched, diastereomerically pure, enantiomerically enriched or enantiomerically pure isomers, or the pharmaceutically acceptable salts and prodrugs thereof to said mammal. The compounds of formula I are growth hormone secretagogues and as such are useful for increasing the level of endogenous growth hormone. In another aspect this invention provides certain intermediates which are useful in the synthesis of the foregoing compounds and certain processes useful for the synthesis of said intermediates and th compounds of formula I. This invention is further directed to methods comprising administering to a human or other animal a combination of a functional somatostatin antagonist such as an alpha-2 adrenergic agonist and a compound of formula I.

专利号:US-7220858-B2
优先权日:2003-12-23
标 题 :Synthesis of hydrazine and chlorinated derivatives of bicyclic pyridazines
发明人：NELSON DEANNA J
权利人:BARBEAU PHARMA INC
摘要:The present invention relates to both a novel method of preparing hydralazine hydrochloride and to a novel method of preparing hydrazine derivatives of compounds containing a pyridazine ring, including, for example, pyridazines, phthalazines and other compounds containing the pyridazine ring.

专利号:US-7244753-B2
优先权日:2002-07-29
标 题:Cyclooxygenase-2 selective inhibitors, compositions and methods of use
发明人：GARVEY DAVID S; KHANAPURE SUBHASH P; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D
权利人:NITROMED INC
摘要:The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal and/or respiratory toxicity; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.