合成目标产物 1-Phenylguanidine 主要起始原料 Cyanamide And Aniline
(文献来源)合成步骤主要原料 Cyanamide 和 Aniline
📜Benzyl N-(N'-Phenyl-N-Phenylmethoxycarbonylcarbamimidoyl)Carbamate置于palladium On Activated Charcoal 氢气体系中,用 甲醇 用作溶剂,化学反应生成苯基胍 参考文献:Urethane Protected Derivatives Of 1-Guanylpyrazole For The Mild And Efficient Preparation Of Guanidines 标题:Urethane Protected Derivatives Of 1-Guanylpyrazole For The Mild And Efficient Preparation Of Guanidines 摘要:Bis-Urethane Protected Derivatives Of 1-Guanylpyrazole Were Prepared And Found To Readily React With Relatively Unreactive Amines At Room Temperature To Produce Bis-Protected Guanidines In Good Yields. Simultaneous Removal Of Both Protecting Groups From These Products Efficiently Produced Monosubstituted Guanidines. Doi:10.1016/s0040-4039(00)79163-5
专利信息
专利号:US-9944593-B2 优先权日:2013-10-04 标 题:Process for the synthesis of fluoralkyl sulfonate salts 发明人:MONZANI CRISTIANO; TORTELLI VITO 权利人:SOLVAY SPECIALTY POLYMERS IT 摘要:A process for the preparation of the fluoroalkyl sulfonate salt of a nitrogen-based organic base said process comprising the step of reacting a fluoroalkyl sulfonyl halide with an organic base selected from the group consisting of tertiary amines, pyridines, amidines and guanidines.
专利号:US-4388310-A 优先权日:1982-03-01 标 题:6-Amido-2-S-oxides of substituted 2-organothio-pen-2-em-3-carboxylic acids 发明人:CHRISTENSEN BURTON G; DININNO FRANK P; MUTHARD DAVID A; RATCLIFFE RONALD W 权利人:MERCK & CO INC 摘要:Disclosed are 6-amido-2-S-oxides of substituted 2-organothio-pen-2-em-3-carboxylic acids (I) which are useful as antibiotics and as intermediates in the synthesis of substituted pen-2-em-3-carboxylic acids: I wherein: R1 is H or acyl; R2 is hydrogen or methoxyl; R3 is alkyl having from 1-6 carbon atoms; phenylalkyl having 7-12 carbon atoms; and cycloalkyl having 3-6 carbon atoms; and R4 is hydrogen, a removable protecting group or a pharmaceutically acceptable salt or ester moiety.
专利号:WO-2011156355-A1 优先权日:2010-06-09 标题 :Production method of phenyl guanidine salts and their intermediates 发明人:JOHNSON MICHAEL ROSS; KANG MYUNG-CHOL; BRAY BRIAN L; SCHNEIDER STEPHEN 权利人:KAINOS MEDICINE INC; JOHNSON MICHAEL ROSS; KANG MYUNG-CHOL; BRAY BRIAN L; SCHNEIDER STEPHEN 摘要:This invention relates to methods for producing phenyl guanidine salts having pharmacological activity, as well as to the identification and synthesis of compounds useful as intermediates for producing phenyl guanidine salts having pharmacological activity.
专利号:US-4171439-A 优先权日:1975-04-11 标 题 :Antibacterial analogs of isocephalosporins 发明人:CONWAY TERRY T; LIM GARY M F; MENARD MARCEL 权利人:BRISTOL MYERS CO 摘要:There is described the stereoselective total synthesis of novel DELTA 2,3-1,4-morpholine-2-carboxylic acids possessing a fused beta -lactam ring in the 1,6-position and carrying a substituent cis to carbon 5 in the 7-position of the fused ring system represented by the general formula I wherein Z is halo or hydroxyl and X is acylamino. Also included in the invention are compounds of the above formula in which the carboxyl group at the 2-position is protected as by an easily cleavable ester group and salts of both the free acids and carboxyl-protected compounds. The compounds are potent antibacterial agents.
专利号:US-5064963-A 优先权日:1990-04-25 标 题 :Process for the synthesis of n-(3-(1h-imidazol-1-yl)phenyl-4-(substituted)-2-pyrimidinamines 发明人:DEAN WILLIAM D 权利人:AMERICAN CYANAMID CO 摘要:The invention provides a novel process for producing N-[3-(1H-imidazol-1-yl)phenyl]-4-(substituted)-2 pyrimidinamine compounds in which the substituent is a 2-pyridinyl, 3-pyrindinyl, 4-pyridinyl, 2-furanyl or 2-thienyl group. The process includes the steps of (1) reacting a 3-(1H-imidazol-1-yl)benzamine with cyanamide and a halogen acid while controlling the pH of the reaction between pH about 2 to abourt 3.5 and recovering a [3-(1H-imidazol-1-yl)phenyl] guanidine dihydrohalide and (2) reacting the [3-(1H-imidazol-1-yl)phenyl] guanidine dihydrohalide so recovered with an appropriately substituted 3-dimethylamino-1-(substituted)-2-propen-1-one and a base at a pH of from about 10.5 to about 11.5 and recovering the N-[3-(1H-imidazol-1-yl)phenyl-4-(substituted)-2-pyrimidamine compound so produced. The novel process provides improved yield and purity by adhering to the stated crucial pH ranges.
专利号:EP-1534734-B1 优先权日:2002-08-30 标题:Method for the synthesis and selective biocatalytic modification of peptides, peptide mimetics and proteins 发明人:BORDUSA FRANK; WEHOFSKY NICOLE; RUDOLPH RAINER 权利人:ROCHE DIAGNOSTICS GMBH; HOFFMANN LA ROCHE 摘要:Method for synthesis and/or selective N-terminal modification of peptides, peptide mimetics and/or proteins (A). Method for synthesis and/or selective N-terminal modification of peptides, peptide mimetics and/or proteins (A) comprises: (1) preparing an amino component (I) containing at least one amino acid (aa); (2) preparing a carboxy component (II) that has a leaving group on carboxy and contains at least one aa, or a marker or reporter group; and (3) reacting (I) and (II) in a medium that contains at least one ionic fluid, in presence of protease, peptidase and/or hydrolase, so that (I) and (II) become linked through a peptide bond, with cleavage of the leaving group.
参考标题:Cui-Catalyzed Amination Of Arylhalides With Guanidines Or Amidines: A Facile Synthesis Of 1-H-2-Substituted Benzimidazoles 作者:Xiaohu Deng,Heather Mcallister,Neelakandha S. Mani |发布日期:2009.8.7 摘要:Cui/l5 (N,N′-Dimethylethylenediamine) Proves To Be An Efficient Catalyst System For The Amination Of Arylhalides With Guanidines. The Same Catalyst System Is Then Successfully Applied To The One-Step Synthesis Of 1-H-2-Amino-Benzimidazoles Through Tandem Aminations Of 1,2-Dihaloarenes In Modest Yields. This Methodology Is Also Applicable For The Preparation Of 1-H Or 1-Substutituted 2-Aryl- Or 2-Alkyl-Benzimidazoles
合成参考文献
摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 143. 摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 193. 摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 213. 摘要:Podlech, J., Science of Synthesis Knowledge Updates, (2019) 1, 410. 摘要:Dornan, P. K.; Dong, V. M., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 1, 161.