247234-41-9

Usage

Uses

Used in Veterinary Medicine:
N-[4-(Morpholin-4-yl)phenyl]guanidine is used as an anthelmintic agent for the treatment of parasitic worm infections in livestock. It is particularly effective against roundworms, hookworms, and whipworms due to its mechanism of action that involves paralyzing the parasites, facilitating their removal from the host's intestinal tract.
Used in Sheep and Cattle Industries:
In the sheep and cattle industries, N-[4-(Morpholin-4-yl)phenyl]guanidine is used as a critical component in maintaining the health of these animals by treating and preventing parasitic worm infestations. Its application helps to ensure the productivity and well-being of the livestock, contributing to the overall efficiency and sustainability of these industries.

Upstream product

• 1027376-20-0 C₂₆H₂₅N₃O₃S 
• 2524-67-6 4-morpholino-4-yl-phenylamine 
• 420-04-2 CYANAMID 
• 100-00-5 4-chlorobenzonitrile 
• 10389-51-2 1-morpholino-4-nitrobenzene 

Downstream Products

• 1159883-57-4 C₂₅H₂₁N₇O₃S 
• 1159883-59-6 N-(3-(5-(2-((4-morpholin-4-ylphenyl)amino)pyrimidin-4-yl)imidazo[2,1-b][1,3]thiazol-6-yl)phenyl)benzamide 
• 945749-71-3 4-(2-(4-(morpholinophenyl)amino)pyrimidin-4-yl)benzoic acid 
• 1056634-68-4 Momelotinib 

Relevant academic research and scientific papers

Synthesis of Imidazoles and Oxazoles via a Palladium-Catalyzed Decarboxylative Addition/Cyclization Reaction Sequence of Aromatic Carboxylic Acids with Functionalized Aliphatic Nitriles

We herein report an efficient approach for the assembly of multiply substituted imidazoles and oxazoles in a single-step manner. These transformations are based on a decarboxylation addition and annulation of readily accessible aromatic carboxylic acids a

Momelotinib preparation method

The invention relates to the field of organic synthesis and preparation of bulk drugs, in particular to an Momelotinib preparation method which comprises the following steps of (1) preparing 4-nitrochlorobenzene and morpholine to obtain 4-(4-nitrophenyl)morpholine, and performing reduction on 4-(4-nitrophenyl)morpholine to prepare 4-morpholinoaniline; (2) performing reaction on 4-morpholinoanilineand cyanamide to prepare 1-(4-morpholinyl phenyl)guanidine; (3) performing reaction on 4-acetylbenzoic acid and glycinonitrile hydrochloride to prepare 4-acetyl-N-(cyanomethyl)benzamide; (4) performing reaction on 4-acetyl-N-(cyanomethyl)benzamide and N,N-dimethylformamide dimethyl acetal to prepare N-(cyanomethyl)-4-(3-(dimethylamino)acryloyl)benzamide; and (5) performing reaction on N-(cyanomethyl)-4-(3-(dimethylamino)acryloyl)benzamide and 1-(4-morpholinyl phenyl)guanidine to prepare the Momelotinib. The method has the characteristics of availability in raw material, concision in technology, convenience in operation, high yield, low cost and the like.

Synthesis and SAR of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as potent and selective CDK4/6 inhibitors

CDK4/6 pathway is an attractive target for development of anti-cancer drugs. Herein, we reported the design and synthesis of a series of 4,5-dihydro-1H-pyrazolo [4,3-h]quinazoline derivatives as selective CDK4/6 inhibitors. Applied with the optimizing strategy to the initial scaffold, it is found that compound 13n is able to selectively inhibit CDK4 and CDK6 with IC50 values 0.01 and 0.026 μM, respectively. The compound showed good anti-proliferative activity when tested in a panel of tumor cell lines with CDK4/6 related mechanism of action, the results clearly suggest that compound 13n works much better than Ly2385219 which is a selective CDK4/6 inhibitor. This compound was also found to have favorable pharmacokinetic parameters. Taken together, compound 13n could be selected for further preclinical evaluation.

New and Practical Synthesis of Momelotinib

New and practical synthetic route of momelotinib, a JAK inhibitor, is described on a decagram scale. A convergent synthetic process is adopted to prepare the methyl 4-(2-((4-morpholinophenyl)amino)pyrimidin-4-yl) benzoate intermediate, by cyclization of 1-(4-morpholinophenyl)guanidine and methyl 4-(3-(dimethylamino)acryloyl)benzoate in high yield and mild conditions. Momelotinib is obtained in 43.2% yield over five steps and 99.1% purity (HPLC).

A novel and efficient synthesis of momelotinib

An improved route for the synthesis of momelotinib has been developed. A nucleophilic addition reaction between the starting material, 4-morpholinoaniline, and cyanamide gave the 1-(4-morpholinophenyl)guanidine. Simultaneously, methyl 4-acetylbenzoate was converted into methyl (E)-4-[3-(dimethylamino)acryloyl]benzoate in the presence of N,N-dimethylformamide dimethylacetal. The enaminone intermediate was then condensed at elevated temperature in alcoholic alkali with the 1-(morpholinophenyl)guanidine to form the desired pyrimidine, which was hydrolysed to the corresponding acid. This procedure is simple in operation, without noble metal catalyst and suitable for industrial production. Finally, the desired compound momelotinib was acquired by an amidation reaction.

A method for preparing Momelotinib JAK inhibitors (by machine translation)

The invention relates to a method for the synthesis of inhibitors JAK Momelotinib, chemical medicine, in the field of chemical engineering and technology. Comprises the following steps : (a) the 4 the aniline and morpholine- [...] 50% shan Jingan dissolve

IMIDAZO-THIAZOLE DERIVATIVES AS PROTEIN KINASE INHIBITORS

Compounds of formula I that inhibit protein kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed. Formula I and therapeutically acceptable salts, prodrugs and salts of prodrugs thereof, wherein X is CH or N; A1 is R1, OR1. NHR1, N(R1)2, NHC(O)R1, NHC(O)NHR1, NHC(O)N(R1)2, NHC(O)OR1, C(O)NHR1, C(O)N(R1)2, C=NOR1, or C(NH2)NOC(O)R1;

Methods and compositions for diagnosing and treating arthritic disorders and regulating bone mass

The present invention relates to improved diagnostic methods for early detection of a risk for developing an arthritic disorder in humans, and screening assays for therapeutic agents useful in the treatment of arthritic disorders, by comparing the levels of one or more indicators of altered mitochondrial function. Indicators of altered mitochondrial function include enzymes such as mitochondrial enzymes and ATP biosynthesis factors. Other indicators of altered mitochondrial function include mitochondrial mass, mitochondrial number and mitochondrial DNA content, cellular responses to elevated intracellular calcium and to apoptogens, and free radical production. Methods of treating, and of stratifying, human patients as such methods relate to disclosed indicators of altered mitchondrial function are also provided.

Solid-phase synthesis of N-aryl-N′-carboalkoxy guanidines by the mitsunobu reaction of Fmoc-guanidines

A new method for the solid-phase synthesis of N-aryl-N′-carboalkoxy guanidines is described. Aromatic amines were reacted with Fmoc-isothiocyanate to provide Fmoc-thioureas, which were coupled with Rink amide resin to provide the corresponding resin-bound Fmoc-guanidines. Subsequent Mitsunobu alkylation with a variety of alcohols delivered N-aryl-N′ carboalkoxy guanidines in good to high purity after resin cleavage.