10191-60-3Relevant articles and documents
Pyrimidine non-nucleoside analogs: A direct synthesis of a novel class of N-substituted amino and N-sulfonamide derivatives of pyrimidines
Elgemeie, Galal H.,Salah, Ali M.,Abbas, Nermeen S.,Hussein, Hoda A.,Mohamed, Reham A.
, p. 213 - 223 (2017)
A convenient method for the regioselective synthesis of pyrimidine non-nucleoside analogs was developed. This study reports a novel and efficient method for the synthesis of a new type of N-substituted amino methylsulfanylpyrimidines and the corresponding pyrazolo[3,4-d]pyrimidines. This series of compounds was designed through the reaction of dimethyl N-cyanodithioiminocarbonate with 2-cyano-N′-(thiophen-2-yl-, furan-2-yl- and pyridin-4-ylmethylene)acetohydrazide and N′-(2-cyanoacetyl)arylsulfonohydrazides. The scope and limitation of the method are demonstrated. The antibacterial and antifungal activities of the synthesized compounds were also evaluated.
Syntheses and Crystal Structures of Methyl N-Substituted-N′-Cyanocarbamimidothioates Derived from Dimethyl N-Cyanodithioiminocarbonate
Wang, Jun-Ling,Ma, Sen,Zhang, Pei-Zhi,Jia, Ai-Quan,Zhang, Qian-Feng
, p. 295 - 302 (2019/07/17)
Abstract: Reaction of dimethyl N-cyanodithioiminocarbonate and arylamine or alkylamine compounds in the refluxing ethanol solution afforded the according methyl N-substituted-N′-cyanocarbamimidothioates 1–16 in good yields. Compounds 1–16 were characterized by proton nuclear magnetic resonance (1H NMR) and infrared spectroscopies, of which the structures of compounds 1, 2 and 3 (Elgemeie et al. in Acta Cryst E71:104–111, 2015) were established by X-ray crystallography, showing that weak hydrogen-bonding interactions exist in compounds 1–3. Compound 1 crystallizes in the orthorhombic space group Pbca, with a = 6.997(2), b = 7.395(2), c = 36.112(11) ?, and Z = 8. The unit cell of 2 has a monoclinic P21/c symmetry with the cell parameters a = 5.8717(12), b = 4.6598(9), c = 37.799(9) ?, β = 91.126(6)°, and Z = 4. Compound 3 crystallizes in the orthorhombic space group Pbca, with a = 7.123(3), b = 7.374(3), c = 38.538(16) ?, and Z = 8. Graphic Abstract: A series of methyl N-subsituted-N′-cyanocarbamimidothioate compounds were efficiently synthesized via the reaction of arylamine or alkylamine compounds with dimethyl N-cyanodithioiminocarbonate. The structures of compounds 1–3 were characterized by X-Ray crystallography.[Figure not available: see fulltext.]
Thiazole amide compound as well as preparation and application thereof
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Paragraph 0007, (2020/08/02)
The invention discloses a thiazole amide compound as well as preparation and application thereof. The structural general formula of the thiazole amide compound is shown in the specification, wherein an X group is selected from methylene (-CH2-), oxygen (O), amino (-NH), N-methyl (-NCH3-), N-isopropyl (-N-CH (CH3) 2) and sulfur (S), and the R group is selected from phenyl, p-methylphenyl, p-nitrophenyl, p-fluorophenyl, p-hydroxyphenyl, p-methoxyphenyl, 3-chloro-2-methylphenyl and 5-chloro-2-methylphenyl. The thiazole amide compound disclosed by the invention has excellent antibacterial activityon valsa mali, fusarium oxysporum, colletotrichum citri and the like, and can be used for preventing and treating crop diseases.
A preparation method of the emetic (by machine translation)
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Paragraph 0027; 0030; 0032; 0037; 0043; 0048; 0053; 0057, (2019/04/17)
The invention relates to the field of organic synthetic technology, in particular to a emetic preparation method, comprises the following steps: S1, 3 - methoxy methyl acrylic acid methyl ester preparation; S2, synthesis of [...]; S3, is the synthesis of third zuo; S4, and aldehyde; S5, closed-loop. This invention adopts the single melamine as the synthetic starting material, greatly reducing the cost, dicyandiamide as to effectively solve the problem of lack of raw material sources; solved in the prior art long reaction time, the reaction condition is sensitive, harsh, side reaction are numerous and complex, the use of expensive or difficult to prepare sodium of other reagents, reactions caused low overall yield, the product quality is poor, so that the synthesis process technology of the route is more stable, good reproducibility, high yield, the product quality is good, content can be up to 99.5%, the yield can reach 85.6%, has higher economic benefits. (by machine translation)
A simple and efficient approach to the synthesis of 1-phosphonated 5-amino-1-H-[1,2,4]-triazole from N-functionalized imidates
Jabli, Dhiab,Dridi, Khaireddine,Efrit, Mohamed Lotfi
, p. 759 - 764 (2016/05/09)
In this study, we describe a new and easy synthetic approach to variously substituted triazoles based on the reaction of imidates with phosphorylated hydrazine in good yields. A general mechanism of the reactions was also proposed. Characterization of the products was carried out by several analytical and spectroscopic tools including infrared and nuclear magnetic resonance spectroscopies (1H,13C NMR,31P NMR).
A convenient synthesis and antimicrobial activity of functionalized 1,2,4-triazoles and 3-amino-alkyltetraazabicyclo[3.3.0]octan-8-ones
Al-Ayed, Abdullah Sulaiman,Dridi, Khaireddine Mohamed
, p. 9233 - 9236 (2013/11/19)
5-Amino-1,2,4-triazole derivatives and their bicyclic system were synthesized in moderate to good yields from the corresponding a-aminoesters, hydrazine or methylhydrazine and the starting material dimethyl N-cyanodithioiminocarbonate. Many target compounds were obtained. But, in cases when the bicyclic system is not formed, 5-amino-1,2,4-triazoles are usually formed. Structures of the prepared compounds were elucidated on the basis of their spectral data and their antifungal and antibacterial activities were also evaluated.
Synthesis of substituted [1,3]thiazolo[4,5-b]pyridines and [1,3]thiazolo[4,5-d][1,2,3]triazines
Thomae, David,Perspicace, Enrico,Hesse, Stéphanie,Kirsch, Gilbert,Seck, Pierre
, p. 9309 - 9314 (2008/12/21)
In this work, we described an easy preparation of substituted 4-amino-5-cyano-1,3-thiazoles. These compounds have been used as starting materials to obtain two classes of compounds. New substituted [1,3]thiazolo[4,5-e]pyridines were synthesized in one step via Friedl?nder reaction. Diazotation of 4-amino-5-cyano-1,3-thiazoles afforded 4-chloro[1,3]thiazolo[4,5-d][1,2,3]triazines in one step. The later was substituted by a secondary amine to obtain substituted 4-amino[1,3]thiazolo[4,5-d][1,2,3]triazines.
ASPARTIC PROTEASE INHIBITORS
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Example 15, (2010/11/27)
The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.
First synthesis of N-substituted amino and N-sulfonylaminated methylthiopyrimidines: Reaction of dimethyl N-cyanodithioiminocarbonate with substituted hydrazides
Elgemeie, Galal H.,Sood, Soha A.
, p. 743 - 753 (2007/10/03)
A novel and efficient method for the synthesis of a new variety of methylsulfanylpyrimidines by the reaction of dimethyl N- cyanodithioiminocarbonate with substituted hydrazides. The synthetic potential of the method is demonstrated. Copyright Taylor & Francis Group, LLC.
Regioselective preparation of N-substituted 3,5-diamino-1,2,4-oxadiazoles
Suyama, Takayuki,Suzuki, Noriyuki,Nishimura, Masami,Saitoh, Yuka,Ohkoshi, Hiroyuki,Yamaguchi, Jun-Ichi
, p. 873 - 876 (2007/10/03)
Regioselective preparation of 3,5-diamino-1,2,4-oxadiazoles which have a substituent on one or the other amino group has been developed. When 1-substituted 3-cyano-2-ethylisourea (2) was allowed to react with hydroxylamine under basic conditions, 5-amino-3-(substituted amino)-1,2,4-oxadiazole (3) was obtained in good yield. On the other hand, 3-amino-5-(substituted amino)-1,2,4-oxadiazoles (4), a regioisomer of 3, could be synthesized by the reaction of N,O-bis(trimethylsilyl)hydroxylamine (9) with 2 or 1-substituted 3-cyano-2-methylisothiourea (1) and subsequent alcoholysis.
