29640-13-9

Upstream product

• 75-44-5 phosgene 
• 1926-80-3 methyl 6-aminocaproate hydrochloride 
• 590-28-3 potassium cyanate 
• 14273-90-6 methyl 6-bromohexanoate 
• 2780-89-4 methyl 6-aminohexanoate hydrochloride 
• 32315-10-9 bis(trichloromethyl) carbonate 

Downstream Products

• 6621-60-9 N,N'-bis(5-methoxycarbonylpent-1-yl)urea 
• 4321-58-8 6-aminohexanoic acid hydrochloride 
• 1129548-00-0 17β-hydroxy-11β-{4-[1-methyl-3-(5-methoxycarbonylpentyl)-ureido]-phenyl}-17α-(1-propinyl)-estra-4,9-dien-3-one 

Relevant academic research and scientific papers

Preparation method and application of iprodione hapten and antigen

The invention provides a preparation method and application of iprodione hapten and antigen. The iprodione hapten is obtained through the following steps: taking 3,5-dichlorophenyl isocyanate and ethyl glycinate hydrochloride to react to generate ethyl 2-(3-(1,5-dichlorophenylcarbamido)) acetate, hydrolyzing to obtain 2-(3-(1,5-dichlorophenylcarbamido))acetic acid, carrying out ring-forming reaction to obtain 3-(3,5-dichlorophenyl)-2,4-imidazolidindione, reacting with methyl 6-isocyanatocaproate generated by reaction of methyl 6-aminohexanoate hydrochloride and triphosgene, so as to generate methyl 6-(3-(3,5-dichlorophenyl)-2,4-dioxyiminazolealkyl-1-formylamino)caproate; finally, hydrolyzing under an acidic condition. The iprodione antigen is obtained by coupling the iprodione hapten and carrier protein. The antigen prepared by the invention has a specific iprodione antigenic determinant, so that a high-specificity iprodione monoclonal antibody is possibly screened. A generated antibody has high specificity and high sensitivity and can be used for enzyme-linked immunization and rapid determination of test paper.

Discovery of N 1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H -pyrrolo[2,3- d] pyrimidin-2-yl)amino)phenyl)- N 8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer

A series of novel, highly potent, selective inhibitors targeting both CDK4/9 and HDAC1 have been designed and synthesized. N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7H-pyrrolo[2,3-d] pyrimidin-2-yl)amino)phenyl)-N8-hydroxyoctanediamide (6e) was discovered. The lead compound 6e with excellent CDK4/9 and HDAC1 inhibitory activity of IC50 = 8.8, 12, and 2.2 nM, respectively, can effectively induce apoptosis of cancer cell lines. The kinase profiling of compound 6e showed excellent selectivity and specificity. Compound 6e induces G2/M arrest in high concentration and G0/G1 arrest in low concentration to prevent the proliferation and differentiation of cancer cells. Mice bared-breast cancer treated with 6e showed significant antitumor efficacy. The insight into mechanisms of 6e indicated that it could induce cancer cell death via cell apoptosis based on CDK4/9 and HDAC1 repression and phosphorylation of p53. Our data demonstrated the novel compound 6e could be a promising drug candidate for cancer therapy.

Synthesis of N-Acylamino-Acid Derivatives of Cytisine

N-acylamino-acid derivatives of cytisine were prepared by reacting cytisine with methyl esters of aminoacid isocyanates.

Aminosaeuren, I. Darstellung von Aminosaeuren aus Halogencarbonsaeure-alkylestern mit Alkalimetallcyanaten

α- and ω-halo- as well as α,ω-dihalocarboxylic alkyl esters react with potassium cyanate in the presence of alcohol at 80 - 120 deg C in dipolar aprotic solvents to yield α- and ω-(alkoxycarbonylamino)- and α,ω-bis(alkoxycarbonylamino)carboxylic alkyl esters, respectively, in good yields.Hydrolytic cleavage of these mono- or diurethanes with an aqueous solution of hydrochloric acid/formic acid leads to the corresponding amino acid hydrochlorides in nearly quantitative yields.