3-氨基苯甲醛置于水 Aluminum Oxide,盐酸羟胺,甲基磺酰氯体系中,化学反应 2.0H,以90%的收率获得3-氨基苯甲酰胺 参考文献:A Direct Synthesis Of Nitriles And Amides From Aldehydes Using Dry Or Wet Alumina In Solvent Free Conditions 标题:A Direct Synthesis Of Nitriles And Amides From Aldehydes Using Dry Or Wet Alumina In Solvent Free Conditions 摘要:An Efficient And Simple Procedure For The Direct Conversion Of Aldehydes Into The Corresponding Nitriles With (Nh2Ohhcl)-H-./dry Al2O3/meso2Cl Or Amides With (Nh2Ohhcl)-H-./wet Al2O3/meso2Cl Are Studied. (C) 2002 Elsevier Science Ltd. All Rights Reserved. Doi:10.1016/s0040-4020(02)01417-5
专利号:US-11427596-B2 优先权日:2019-07-19 标 题:Metal-free solvent-free synthesis of fused-pyrido heterocycles and biomedical applications 发明人:CHELVAM VENKATESH; DUDHE PREMANSH; KRISHNAN MENA ASHA; SONAWANE AVINASH 权利人:INDIAN INSTITUTE OF TECH INDORE 摘要:Embodiments herein provide fused-pyrido heterocycles such as azaindoles, carboline derivatives, furo[b]pyridines or furo[b]pyridine-isatin hybrids of Formula I.Embodiments also relate to a process for a synthesis of variety of complex pyrido-heterocycles The pyrido-heterocycles can be used for treating cancer (cervix, kidney, lung, breast and epidermal skin) and multi-drug resistant tuberculosis. These heterocycles can also be used as anti-biofilm agents against pathogenic strains, which will minimize the risk of secondary infections.
专利号:US-5763625-A 优先权日:1995-04-25 标 题:Synthesis and use of β-lapachone analogs 发明人:BOOTHMAN DAVID A; FRYDMAN BENJAMIN J; WITIAK DONALD T 权利人:WISCONSIN ALUMNI RES FOUND 摘要:3-Substituted-β-lapachone analogs and their use either alone or to augment chemotherapy or radiotherapy to induce programmed neoplastic cell death without exhibiting toxicity to surrounding normal cells are disclosed. In particular, 3-allyl-β-lapachones, 3-alkyl-β-lapachones and 3-halo-β-lapachones were found to be Topoisomerase (Topo I) inhibitors. When these analogs are used alone there is a reversible single-strand break in the DNA of neoplastic cells causing apoptosis and cell death in some cells. However, when these analogs are combined with chemotherapy or X-irradiation, an irreversible Topo I-mediated break is achieved. A new and more efficient chemical synthesis of the compounds is also disclosed.
专利号:US-12043612-B2 优先权日:2020-05-09 标 题 :Methods of manufacturing a bifunctional compound, ultrapure forms of the bifunctional compound, and dosage forms comprising the same 发明人:ALLAN LAURA E N; CHEN CHUNGPIN HERMAN; DONG HANQING; GROSSO JOHN A; HASKELL III ROYAL J; LLOYD RHYS; REECE HAYLEY 权利人:ARVINAS OPERATIONS INC 摘要:The present disclosure relates to ultra-pure forms, polymorphs, amorphous forms, and formulations of N-[(1r,4r)-4-(3-chloro-4-cyanophenoxy)cyclohexyl]-6-[4-({4-[2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl]piperazin-1-yl}methyl)piperidin-1-yl]pyridazine-3-carboxamide, referred to herein as Compound A:The present disclosure also relates methods of manufacturing and purifying the same, as well as intermediates useful in the synthesis of Compound A. The ultra-pure forms, polymorphs, amorphous forms, and formulations of Compound A can be used as therapeutic agents for the treatment of various diseases and conditions such as cancer.
专利号:US-10772971-B2 优先权日:2017-06-22 标 题:Methods of producing drug-carrying polymer scaffolds and protein-polymer-drug conjugates 发明人:GURIJALA VENU REDDY; BOLLU SATYANARAYAN REDDY; LEBLANC JACQUES; LOWINGER TIMOTHY B; MCGILLICUDDY DENNIS; YIN MAO; YURKOVETSKIY ALEKSANDR V 权利人:MERSANA THERAPEUTICS INC; MERSANA THERPEUTICS INC 摘要:The disclosure provides methods of synthesis of polymeric scaffolds, e.g., those useful for conjugating with a protein based recognition-molecule (PBRM) to form PBRM-polymer-drug conjugates, and PBRM-polymer-drug conjugates thereof. The methods according to the disclosure allow for large-scale preparation of polymeric scaffolds having a high purity. In some embodiments, the methods according to the disclosure also allow for the preparation of scaffolds and conjugates thereof in better yield than previously used methods for preparing same. Also disclosed are methods of purifying polymeric scaffolds.
专利号:US-9365532-B1 优先权日:2011-02-14 标题:Synthesis, composition and use of novel therapeutic and cosmetic Schiff base products formed by reaction of a carbonyl containing moeity with a transimination nucleophilic catalyst and the use of transimination nucleophilic catalysts to increase the rate at which carbonyl containing therapeutic and cosmetic actives form Schiff base products with biological amines 发明人:ISAACMAN STEVEN 权利人:ISAACMAN STEVEN; NANOMETICS LLC 摘要:The present invention relates to the synthesis, composition and use of novel moieties formed by reacting a transimination nucleophilic catalyst, molecular or polymeric, with carbonyl-containing therapeutic or cosmetic moieties. The resultant Schiff base product is highly reactive towards transimination with a biological amine. The catalyst and carbonyl-containing moiety can be molecular or polymeric, and the resultant chemical and physical properties of the Schiff base products can be engineered by appropriate selection of said catalyst. The present invention also relates to the synthesis, composition and use of novel moieties that are used as actives in sunless tanning preparations. The present invention also relates to the use of transimination nucleophilic catalysts to increase the rate at which a carbonyl-containing moiety reacts with a biological amine. The present invention also relates to the use of transimination nucleophilic catalysts to increase the rate and efficacy of commercial sunless tanning preparations. Improvements on stability and efficacy of said preparations are disclosed. While the invention has been described in terms of its preferred embodiments, those skilled in the art will recognize that the invention can be practiced with modification within the spirit and scope of the appended claims. Accordingly, the present invention should not be limited to the embodiments as described above, but should further include all modifications and equivalents thereof within the spirit and scope of the description provided herein.
专利号:US-2003120355-A1 优先权日:2001-06-08 标题 :Biocompatible and biodegradable polymers for diagnostic and therapeutic radioisotope delivery 发明人:HAFELI URS; RUDERSHAUSEN SANDRA; TELLER JOACHIM; GRUTTNER CORDULA 摘要:This invention relates to biocompatible and biodegradable polymers which are able to bind diagnostic and therapeutic radioisotopes, and the therapeutic use of the same as well as the synthesis of such polymers. It further relates to the preparation of functional implants from these materials, including nanospheres, microspheres, liposomes, micelles, coatings, films, fibers, and foils.
[参考文献]: Brock Wa, Et Al. Radiosensitization Of Human And Rodent Cell Lines By Ino-1001, A Novel Inhibitor Of Poly(Adp-Ribose) Polymerase. Cancer Lett. 2004 Mar 18;205(2):155-60. [参考文献]: Clark Rs, Et Al. Local Administration Of The Poly(Adp-Ribose) Polymerase Inhibitor Ino-1001 Prevents Nad+ Depletion And Improves Water Maze Performance After Traumatic Brain Injury In Mice. J Neurotrauma. 2007 Aug;24(8):1399-405. [参考文献]: Radovits T, Et Al. Poly(Adp-Ribose) Polymerase Inhibition Improves Endothelial Dysfunction Induced By Reactive Oxidant Hydrogen Peroxide In Vitro. Eur J Pharmacol. 2007 Jun 14;564(1-3):158-66. [参考文献]: Szabo C, Et Al. Poly(Adp-Ribose) Polymerase Inhibitors Ameliorate Nephropathy Of Type 2 Diabetic Leprdb/db Mice. Diabetes. 2006 Nov;55(11):3004-12. [参考文献]: Baomin Feng, Et Al. Protein Poly(Adp-Ribosyl)Ation Regulates Arabidopsis Immune Gene Expression And Defense Responses. Plos Genet. 2015 Jan 8;11(1):E1004936.
合成参考文献
摘要:Klapars, A., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 216. 摘要:Hay, M. B.; Hicks, J. D., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 114. 摘要:Archives of Environmental Contamination and Toxicology., 12(355), 1983 [] 摘要: 摘要:Full text: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC361090