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-12102615-B2 优先权日:2018-04-05 标 题:Synthesis of novel xylose free occidiofungin analogues and methods of using them 发明人:SMITH JAMES L; GENG MENGXIN; RAVICHANDRAN AKSHAYA; ORUGUNTY RAVI 权利人:TEXAS A & M UNIV SYS; SANO CHEMICALS 摘要:The subject invention pertains to methods for producing novel occidiofungin analogues lacking xylose (OF-Δxyl analogue). OF-Δxyl analogues can contain aldehyde, amine, triazole, or hydrazones. The aldehyde, amine, triazole or hydrazone containing analogues of OF-Δxyl can be further modified by substitution with additional functional groups. Various OF-Δxyl analogues described herein have reduced inflammation and toxicity and superior pharmacological properties compared to the natural occidiofungins. Accordingly, certain embodiments of the invention provide methods of treating or preventing fungal infections by administering to the subjects in need thereof the OF-Δxyl analogues described herein.
专利号:US-5877296-A 优先权日:1994-06-03 标题:Process for preparing conjugates of methyltrithio antitumor agents 发明人:HAMANN PHILIP ROSS; HINMAN LOIS; HOLLANDER IRWIN 权利人:AMERICAN CYANAMID CO 摘要:This invention describes carrier-drug conjugates prepared from disulfide analogs of the calicheamicin family of potent antitumor antibiotics and their derivatives, as well as similar analogs from related antitumor antibiotics such as the esperamicins. The carrier can be an antibody, growth factor, or steroid which targets an undesired population of cells, such as those of a tumor. Whole protein carriers as well as their antigen-recognizing fragments and their chemically or genetically manipulated counterparts are useful for the targeting portion of the conjugates. This invention includes compounds required for the synthesis of these conjugates, appropriate pharmaceutical compositions of the carrier-drug conjugates, and their method of use.
专利号:US-5233044-A 优先权日:1989-06-08 标题:Active esters for solid phase peptide synthesis 发明人:HUDSON DEREK 权利人:MILLIPORE CORP 摘要:Derivatives of 1-phenyl pyrazolin-5-one have many applications for biomolecule synthesis. Enol esters of protected amino acids made by the present process provide efficient coupling in solid-phase peptide synthesis. The 1-phenyl-pyrazolin-5-one derivatives are highly crystalline, stable, non-toxic and easy to prepare. Many possess self-indicating properties, facilitating spectrophotometric monitoring and automation of peptide synthesis.
专利号:EP-0401797-A1 优先权日:1989-06-08 标 题:Active esters for solid phase peptide synthesis 发明人:HUDSON DEREK 权利人:MILLIPORE CORP 摘要:Derivatives of 1-phenyl pyrazolin-5-one have many applications for biomolecule synthesis. Enol esters of protected amino acids made by the present process provide efficient coupling in solid-phase peptide synthesis. The 1-phenyl-pyrazolin-5-one derivatives are highly crystalÂline, stable, non-toxic and easy to prepare. Many possess self-indicating properties, facilitating spectroÂphotometric monitoring and automation of peptide synthesis.
专利号:US-7186709-B2 优先权日:2002-08-27 标 题:Dihydropyrancarboxamides and uses thereof 发明人:SCHREIBER STUART L; STAVENGER ROBERT A; MITCHISON TIMOTHY J; MALIGA ZOLTAN 权利人:HARVARD COLLEGE 摘要:The present invention provides novel dihydropyrancarboxamide compounds of formula (I): n nand collections of these compounds, and provides methods for the synthesis of these compounds; wherein R 1 –R 6 are as defined herein. Additionally, the present invention provides pharmaceutical compositions and methods for treating disorders such as proliferative diseases, and cancer, to name a few.
参考标题:A Novel Method For The Synthesis Of 1(2H)- Phthalazinone Derivatives Using Heteropolyacids As Heterogeneous And Recyclable Catalysts 作者:Majid M. Heravi,Bita Baghernejad,Hossein A. Oskooie,Fatemeh F. Bamoharram |发布日期:2008.1 摘要:A Simple And Efficient Synthesis Of 1(2H)Phthalazinone Derivatives Was Achieved Via A Reaction Of Phthalaldehydic Acid And Various Phenyl Hydrazines In Chci3 In The Presence Of A Catalytic Amount Of Different Heteropolyacids (Hpas) In Very Good Yields.
合成参考文献
摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 129. 摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 138. 摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 113. 摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 109. 摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 117.