CAS: 619-67-0; 4-Hydrazinylbenzoic Acid

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4-amino-benzoic acid 4-Bromobenzoic acid 4-hydrazinobenzoic acid hydr°Chloride 4-([4]pyridylmethylene-hydrazino)-benzoic acid 6,7,8,9-tetrahydro-5H-carbazole-3-carboxylic acid 4-cyclohexylidenehydrazino-benzoic acid 1-(4-carboxyphenyl)-3-methyl-5-pyrazolone

对氨基苯甲酸置于盐酸,Sodium Nitrite,Clh*cl2Sn体系中,用 水 作为反应溶剂,化学反应 0.67H,反应生成 4-肼基苯甲酸
参考文献:通过活性导向组合化学合成策略发现新型人磷酸甘油酸脱氢酶抑制剂
标题:通过活性导向组合化学合成策略发现新型人磷酸甘油酸脱氢酶抑制剂
摘要:丝氨酸是从头合成嘌呤和脱氧胸苷所必需的一碳单元的来源,在癌细胞的生长中起着至关重要的作用.磷酸甘油酸脱氢酶 (Phgdh) 催化丝氨酸从头生物合成中的第一个限速步骤,已成为治疗癌症的有希望的靶点.在这里,我们从基于酶促测定的内部小分子库的筛选中确定了h-G6作为潜在的 Phgdh 抑制剂.我们采用了活性导向的组合化学合成策略来优化这种命中化合物.发现化合物b36是非竞争性和最有前途的化合物,其对 Phgdh 的ic 50值为 5.96 +/-0.61 μm.化合物b36抑制人乳腺癌和卵巢癌细胞的增殖,减少细胞内丝氨酸合成,破坏dna合成,并诱导细胞周期停滞.总的来说,我们的结果表明b36是一种新型的 Phgdh 抑制剂,它可能是一种有前景的调节丝氨酸合成途径的调节剂,并且可能是一种潜在的抗癌先导物,值得进一步探索.
DOI:10.1016/j.Bioorg.2021.105159

专利信息

专利号:US-11040938-B2
优先权日:2016-07-27
标 题 :Continuous flow process for the synthesis of phenylhydrazine salts and substituted phenylhydrazine salts
发明人：MA BING; PAN SHUAI
权利人:SHANGHAI HYBRID—CHEM TECH; SHANGHAI HYBRID CHEM TECH
摘要:The present invention provided a continuous flow process for the synthesis of phenylhydrazine salts and substituted phenylhydrazine salts. Diazotization, reduction, acidic hydrolysis and salifying with acids are innovatively integrated together. Using acidic liquids of aniline or substituted aniline, diazotization reagents, reductants and acids as raw materials, phenylhydrazine derivative salts is obtained through the synthesis process, which is a three-step continuous tandem reaction including diazotization, reduction, acidic hydrolysis and salifying. The described synthesis process is a kind of integrated solutions, which is carried out in an integrated reactor. The feed inlets of the integrated reactor are continuously filled with raw materials. In the integrated reactor, diazotization, reduction, acidic hydrolysis and salifying are carried out continuously and orderly, and phenylhydrazine salts or substituted phenylhydrazine salts is obtained in the outlet of the integrated reactor without interruption. The total reaction time is no more than 20 min.

专利号:US-8907083-B2
优先权日:2010-08-25
标题 :Process for the preparation, of 2-(2-hydroxyphenyl)-benz [1, 3] oxazin-4-one and its use for preparation of 4-[3, 5-bis (2-hydroxyphenyl)-IH-I, 2, 4-triazolTI-yl] benzoic acid
发明人：DAVULURI RAMAMOHAN RAO; PONNAIAH RAVI; BATTHNI GURUSWAMY; MEDIDA CHANDRA MURTHY V R; DUMMU SANTHOSH
权利人:DAVULURI RAMAMOHAN RAO; PONNAIAH RAVI; BATTHNI GURUSWAMY; MEDIDA CHANDRA MURTHY V R; DUMMU SANTHOSH; RAMAMOHAN RAO DAVULURI
摘要:The invention provides a novel process for the synthesis of 2-(2-hydroxyphenyl)-benz[1,3]oxazin-4-one, the process comprising of reacting the salicylic acid with salicylamide in the presence of p-toluenesulfonyl chloride, base and solvent. The use of 2-(2-hydroxyphenyl)-benz[1,3]oxazin-4-one in the preparation of Deferasirox is also disclosed in the invention.

专利号:US-8147799-B2
优先权日:2007-01-11
标题:Methods and compositions for improved F-18 labeling of proteins, peptides and other molecules
发明人：MCBRIDE WILLIAM J; GOLDENBERG DAVID M
权利人:MCBRIDE WILLIAM J; GOLDENBERG DAVID M; IMMUNOMEDICS INC
摘要:The present application discloses compositions and methods of synthesis and use of F-18 labeled molecules of use, for example, in PET imaging techniques. In particular embodiments, the labeled molecules may be peptides or proteins, although other types of molecules including but not limited to aptamers, oligonucleotides and nucleic acids may be labeled and utilized for such imaging studies. In preferred embodiments, the F-18 label may be conjugated to a targeting molecule by formation of a metal complex and binding of the F-18-metal complex to a chelating moiety, such as DOTA, NOTA, DTPA, TETA or NETA. In other embodiments, the metal may first be conjugated to the chelating group and subsequently the F-18 bound to the metal. In other preferred embodiments, the F-18 labeled moiety may comprise a targetable conjugate that may be used in combination with a bispecific or multispecific antibody to target the F-18 to an antigen expressed on a cell or tissue associated with a disease, medical condition, or pathogen. Exemplary results show that F-18 labeled targetable conjugate peptides are stable in human serum at 37° C. for several hours, sufficient time to perform PET imaging analysis.

专利号:US-8153100-B2
优先权日:2007-01-11
标题 :Methods and compositions for F-18 labeling of proteins, peptides and other molecules
发明人：MCBRIDE WILLIAM J; D SOUZA CHRISTOPHER A; GOLDENBERG DAVID M
权利人:MCBRIDE WILLIAM J; D SOUZA CHRISTOPHER A; GOLDENBERG DAVID M; IMMUNOMEDICS INC
摘要:The present application discloses compositions and methods of synthesis and use of 18 F or 19 F labeled molecules of use in PET or MRI imaging. The labeled molecules may be peptides or proteins, although other types of molecules may be labeled. Preferably, the 18 F or 19 F is conjugated to a targeting molecule by formation of a metal complex and binding of the 18 F- or 19 F-metal complex to a chelating moiety. Alternatively, the metal may first be conjugated to the chelating group and subsequently the 18 F or 19 F bound to the metal. In other embodiments, the 18 F or 19 F labeled moiety may comprise a targetable construct used in combination with a bispecific antibody to target a disease-associated antigen. The 18 F or 19 F labeled targetable construct peptides are stable in serum at 37° C. for a sufficient time to perform PET or MRI imaging.

专利号:US-9469850-B2
优先权日:2007-01-18
标 题 :Oligosaccharides comprising an aminooxy group and conjugates thereof
发明人：ZHU YUNXIANG; CHENG SENG H; JIANG CANWEN; AVILA LUIS Z
权利人:GENZYME CORP
摘要:The invention provides methods for the synthesis of oligosaccharides comprising an aminooxy group. The invention further provides oligosaccharides comprising an aminooxy group, methods for coupling oligosaccharides comprising an aminooxy group to glycoproteins, and oligosaccharide-protein conjugates. Also provided are methods of treating a lysosomal storage disorder in a mammal by administration of an oligosaccharide-protein conjugate.

专利号:US-8147800-B2
优先权日:2007-01-11
标 题 :Methods and compositions for F-18 labeling of proteins, peptides and other molecules
发明人：MCBRIDE WILLIAM J; D SOUZA CHRISTOPHER A; GOLDENBERG DAVID M
权利人:MCBRIDE WILLIAM J; D SOUZA CHRISTOPHER A; GOLDENBERG DAVID M; IMMUNOMEDICS INC
摘要:The present application discloses compositions and methods of synthesis and use of F-18 labeled molecules of use, for example, in PET imaging techniques. The labeled molecules may be peptides or proteins, although other types of molecules may be labeled by the described methods. Preferably, the F-18 may be conjugated to a targeting molecule by formation of a metal complex and binding of the F-18-metal complex to a chelating moiety. Alternatively, the metal may first be conjugated to the chelating group and subsequently the F-18 bound to the metal. In other embodiments, the F-18 labeled moiety may comprise a targetable construct used in combination with a bispecific or multispecific antibody to target F-18 to a disease-associated antigen, such as a tumor-associated antigen. The F-18 labeled targetable construct peptides are stable in serum at 37° C. for a sufficient time to perform PET imaging analysis.