其它别名Patent Blue VF; Sulfan Blue; Food Blue 3; N-[4-[[4-(Diethylamino)phenyl](2,4-disulfophenyl)methylene]-2,5-cyclohexadien-1-ylidene]-N-ethyl-ethanaminium inner salt sodium salt
专利号:US-2005080260-A1 优先权日:2003-04-22 标 题 :Preparation of prodrugs for selective drug delivery 发明人:MILLS RANDELL L; WU GUO-ZHANG 摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.
专利号:US-3681297-A 优先权日:1970-11-10 标 题 :Synthesis of polybenzothiazolines and polybenzothiazoles by reacting a dialdehyde with an aromatic bis-mercaptoamine 发明人:ALELIO GAETANO FRANCIS D 权利人:GAETANO FRANCIS D ALELIO 摘要:THIS INVENTION DEALS WITH A NOVEL, RELATIVELY SIMPLE PROCESS OF PREPARING POLYBENZOTHIAZOLINES, ((-NH-CH(-)-S-)>AR<(-NH-CH(-Z(-))-S-))N BY REACTING DIALDEHYDES, Z-(CH=O)2, AND (HS)2-AR(-NH2)2 IN A SOLVENT IN AN INERT ATMOSPHERE AND THEREAFTER OXIDIZING THE POLYBENZOTHIAZOLINES TO POLYBENZOTHIAZOLES, ((-N=C(-)-S-)>AR<(-N=C(-Z(-))-S-))N WHEREIN AR REPRESENTS A TETRAVALENT AROMATIC MOIETY IN WHICH THE NITROGEN AND SULFUR ATOMS IN EACH PAIR ARE DISPOSED ORTHO TO EACH OTHER AND Z REPRESENTS A DIVALENT HYDROCARBON MOIETY AS THE RESIDUE OF THE DIALDEHYDE, Z(CHO)2. NEW TYPES, AS WELL AS THE KNOW TYPES OF POLYBENZOTHIAZOLES HAVE BEEN PREPARED BY THIS PROCESS.
专利号:US-5262331-A 优先权日:1989-08-28 标 题 :Method for monitoring in peptide synthesis 发明人:SALISBURY STEPHEN; TREMEER JOHN; OWEN DAVID; DAVIES JOHN 权利人:SALISBURY STEPHEN; TREMEER JOHN; OWEN DAVID; DAVIES JOHN 摘要:A method for monitoring the reaction between an activated carboxylic acid derivative and an amine, such as the formation of a peptide bond in peptide synthesis, whereby an inert anionic dye component and an inert cationic component are included in the reaction system, in small relative amounts compared to the carboxylic acid derivative. The distribution of the dye component to the cationic component, when separated from the amine component, is monitored and at a given maximum value indicates a substantially quantitative reaction.
专利号:US-12180142-B1 优先权日:2024-02-22 标 题:Synthesis process for high purity isosulfan blue using flash chromatography in commercial plant scale 发明人:KAVURU VIMAL; PATI KAMALKISHORE 权利人:RISING PHARMA HOLDINGS INC 摘要:A composition including a N-[4-[[4-(diethyl amino) phenyl](2,5-disulfophenyl)methylene]-2,5-cyclohexadien-1-ylidene]-N-ethylethanaminium sodium salt, where the N-4-4-(diethylamino)phenyl (2,5-disulfophenyl)methylene-2,5-cyclohexadien-1-ylidene-N-ethylethanaminium sodium salt is at least 90% of the weight of such composition. A method of making the composition by a process including sulphonating 2-chlorobenzaldehyde, treatment with sodium sulphite and subsequent basification, a condensation step, an oxidation step and a purification step comprising utilizing HPLC to monitor the sulphonating step, the treatment step, the condensation step, and/or the oxidation step, to determine when one or more reactions of such sulphonating step, treatment step, condensation step, and/or oxidation step are substantially complete and ending such one or more reactions on the basis of the HPLC monitoring. The purification step utilizes flash chromatography to obtain a high purity N-[4-[[4-(diethyl amino) phenyl](2,5-disulfophenyl)methylene]-2,5-cyclohexadien-1-ylidene]-N-ethylethanaminium sodium salt.
专利号:US-2002039652-A1 优先权日:1996-04-29 标题:Synthesis of alumina acetate monohydrate salt sol fibers and uses thereof
专利号:US-2020123103-A1 优先权日:2017-05-12 标 题 :Method for the synthesis of an n-acyl compound without the use of organic solvent or acid chloride
[参考文献]: Barranger E, Et Al. Laparoscopic Sentinel Lymph Node Procedure Using A Combination Of Patent Blue And Radioisotope In Women With Cervical Carcinoma. Cancer. 2003 Jun 15;97(12):3003-9. [参考文献]: Mennel S, Et Al. Patent Blue: A Novel Vital Dye In Vitreoretinal Surgery. Ophthalmologica. 2006;220(3):190-3. [参考文献]: Benoit Ayestaray, Et Al. Patent Blue-Enhanced Lymphaticovenular Anastomosis. J Plast Reconstr Aesthet Surg. 2013 Mar;66(3):382-9. [参考文献]: Daniel Kiblboeck, Et Al. A Misguided 'Pill In The Pocket' Approach With Flecainide Leading To Cardiac Arrest. Bmj Case Rep. 2012 Aug 27:2012:Bcr2012006868. [参考文献]: David Pavlista, Et Al. Relationship Between The Lymphatic Drainage Of The Breast And The Upper Extremity: A Postmortem Study. Ann Surg Oncol. 2012 Oct;19(11):3410-5.
合成参考文献
摘要:Gigiena Truda i Professional'nye Zabolevaniya. Labor Hygiene and Occupational Diseases., 7(2)(54), 1963 摘要:Scientia Pharmaceutica., 47(39), 1979 摘要:NIOSH; National Occupational Exposure Survey (NOES) (1983) 摘要:Franke C et al; Chemosphere 29: 1501-14 (1994) 摘要:Baughman GL, Perenich TA; Amer Dyestuff Reporter p. 19-22. February (1988)