6522-91-4

Upstream product

• 62-53-3 aniline 
• 4023-02-3 1H-pyrazole-1-carboximidamide hydrochloride 
• 110235-27-3 4,6-dimethoxy-N-phenylpyrimidin-2-ylamine 
• 108-86-1 bromobenzene 
• 152120-56-4 N,N′-bis(tert-butoxycarbonyl)-N′′-phenylguanidine 

Downstream Products

• 102-06-7 diphenylguanidine 
• 5199-82-6 N-Chlor-N'-phenyl-guanidin 
• 100185-43-1 2-Amino-1-phenyl-5,6-dihydro-4(1H)-pyrimidinon 
• 39536-03-3 N-(phenylcarbamothioyl)benzenecarboximidamide 
• 100185-44-2 1-(3-Ethoxypropionyl)-3-phenylguanidin 
• 2002-16-6 1-phenylguanidine 

Relevant academic research and scientific papers

Ultrasound-assisted synthesis of substituted guanidines using 1H-pyrazole-1-carboxamidine and S-methylisothiouronium sulfate under solvent-free conditions

We have investigated ultrasound-assisted synthesis of guanidine derivatives using 1H-Pyrazole-1-carboxamidine (PyzCA) and S-substituted isothiouronium sulfate (MeITU). The guanylations of several amines are promoted by ultrasound sonication under solvent-free conditions, and proceed under mild conditions. It is of particular interest that the guanylations do not require bases in most cases.

Cleavage of 2-(Arylamino)-4,6-dimethoxypyrimidines to yield arylguanidines

A novel method for the synthesis of aryl-substituted guanidines in good overall yields is presented; it consists of the acidic cleavage of 2-(arylamino)-4,6-dimethoxypyrimidines, which were prepared by coupling aryl bromides with 2-amino-4,6-dimethoxypyrimidine. This methodology introduces a new means of protection for the guanidine functionality. Copyright

GUANIDINE BASED COMPOUNDS

The adrenergic receptors or adrenoceptors are a family of G-protein coupled receptors split into α and β subclasses. The adrenoceptors have important roles in regulating a myriad of physiological conditions and their malfunction has been implicated in the pathophysiology of a number of diseases. Disclosed herein are a series of novel guanidine and 2-aminoimidazoline compounds which are ligands of the alpha2-adrenoceptor (α2-ARs) subclass of adrenergic receptors. The invention also provides for pharmaceutical compositions comprising the novel compounds. The compounds are suitable for use in the manufacture of medicaments for the treatment of α2-ARs associated disorders, such as depression, schizophrenia, glaucoma and analgesia.

Guanidine and 2-aminoimidazoline aromatic derivatives as α2-adrenoceptor antagonists. 2. Exploring alkyl linkers for new antidepressants

The preparation of a number of (bis)guanidine and (bis)2-aminoimidazoline derivatives as potential α2-adrenoceptor antagonists for the treatment of depression is presented. Human brain tissue was used to measure their affinity toward the α2-adrenoceptors in vitro. Compounds 6b, 8b, 9b, 10b, 15b, 17b, 18b, 20b, and 21b displayed a good affinity (pK i > 7) and were evaluated in in vitro functional [ 35S]GTPγS binding assays in human prefrontal cortex to determine their agonistic or antagonistic activity. Among these compounds, 17b and 20b showed the expected behavior for an antagonist and were subject to in vivo microdialysis experiments in rats. Significantly, these experiments confirmed the antagonistic properties of 17b and 20b, and therefore both compounds can be considered as potential antidepressants.

New cellulose-supported reagent: A sustainable approach to guanidines

(Chemical Equation Presented) A new cellulose-supported reagent for the synthesis of guanidine in aqueous medium is reported starting from commercially available functionalized cellulose beads. Primary and secondary amines, anilines, and amino acids were transformed to the corresponding guanidines in high yields and under very mild conditions.

Total deprotection of N,N'-bis(tert-butoxycarbonyl)guanidines using SnCl4

The total deprotection of NdV'-bis-Boc guanidines using SnCl4 proceeds smoothly in ethyl acetate at room temperature and leads to the easily isolable corresponding guanidinium chlorides.

Process for the manufacture of guanidines

A process for the manufacture of a guanidine by amidination of a primary or secundary amine, which process comprises reacting the amine with a salt of 1-amidino-1,2,4-triazol with a strong acid.