Tag: M.W=150-200

Kobe, J. published the artcileSynthesis of pyridazine derivatives. XV. Electrophilic substitutions on imidazo[1,2-b]pyridazines, Application In Synthesis of 18087-75-7, the main research area is SUBSTITUTION IMIDAZO PYRIDAZINES; IMIDAZOPYRIDAZINES; PYRIDAZINES IMIDAZO.

Imidazo[1,2-b]pyridazine (I), which was prepared for the first time, and several of its analogs were submitted to electrophilic substitution, such as halogenation, nitration and sulfonation. N.M.R. data for several imidazo[1,2-b]pyridazines are included and from these conclusive evidence is obtained that electrophilic substitution occurs at position 3. 17 references.

Tetrahedron published new progress about SUBSTITUTION IMIDAZO PYRIDAZINES; IMIDAZOPYRIDAZINES; PYRIDAZINES IMIDAZO. 18087-75-7 belongs to class pyridazine, name is 3-Nitroimidazo[1,2-b]pyridazine, and the molecular formula is C6H4N4O2, Application In Synthesis of 18087-75-7.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Crossland, Ingolf published the artcileDihydropyridazines. XII. Stereochemical course of protonation of pyridazine Grignard adducts, Synthetic Route of 7145-60-0, the main research area is pyridazine Grignard adduct conformation.

Three Grignard-pyridazine adducts (I,R = Me3C, R1 = MeO; R = Ph R1 = MeO; R = Me3C, R1 = Me2N) were prepared The chem. shifts and coupling constants of the 3 ring protons of I were determined and compared with the deuterated analogs. The results showed that the proton introduced during hydrolysis assumed a pseudoaxial position and thus was identical with the proton introduced by base-catalyzed exchange of II(R2 = Me3C and Ph).

Acta Chemica Scandinavica (1947-1973) published new progress about pyridazine Grignard adduct conformation. 7145-60-0 belongs to class pyridazine, name is 6-Chloro-N,N-dimethylpyridazin-3-amine, and the molecular formula is C6H8ClN3, Synthetic Route of 7145-60-0.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Assandri, A. published the artcileMetabolic pathways of the antihypertensive agent, N-(2,5-dimethyl-1H-pyrrol-1-yl)-6-(4-morpholinyl)-3-pyridazinamine hydrochloride. I. Studies in the rat, Quality Control of 17259-32-4, the main research area is MDL 899 metabolism; pyrrolylpyridazinamine metabolism.

The metabolic fate of a new antihypertensive, MDL 899 (I) [86703-02-8] was studied in rats after both oral and i.v. administration (1 mg/kg). The compound underwent rapid metabolism, disappearing from the central compartment with a half-life of about 0.5 h. Plasma concentration of the parent drug and its major metabolite II  [100499-32-9] following i.v. and oral administration suggest a route-dependent first-pass metabolism Ten metabolites were isolated from the urine and identified by u.v., i.r., mass and 1H NMR spectroscopy. The structure of some was confirmed by 13C NMR and chem. synthesis. All biotransformations are restricted to the pyrrole ring which undergoes oxidative cleavage followed by a series of chem. rearrangements. A minor pathway leads to the formation of Me sulphinyl and Me sulfonyl pyrroles. It is suggested that, as with natural indoles, the pyrrole might be oxidized by a 2,3-dioxygenase. All metabolites tested (3 major and 2 minor) failed to showed antihypertensive activity in spontaneously hypertensive rats.

Xenobiotica published new progress about MDL 899 metabolism; pyrrolylpyridazinamine metabolism. 17259-32-4 belongs to class pyridazine, name is 4-(6-Chloropyridazin-3-yl)morpholine, and the molecular formula is C8H10ClN3O, Quality Control of 17259-32-4.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Cookson, R. F. published the artcileBasicities of pyridazine derivatives, Application of 6-Chloro-N,N-dimethylpyridazin-3-amine, the main research area is Hammett basicity pyridazine; pyridazone oxygen protonation Hammett; protonation pyridazine mechanism.

The Hammett free-energy relation was used to correlate the differences in basicity of six 3-(dimethylamino)pyridazines, five 3-chloropyridazines, and seven 3-pyridazones with substituent constants; protonation occurred ortho to the Me2N group of the (dimethylamino)pyridazines, meta to the Cl of the chloropyridazines, and on the exocyclic O of the pyridazones.

Journal of the Chemical Society, Perkin Transactions 9: Physical Organic Chemistry published new progress about Hammett basicity pyridazine; pyridazone oxygen protonation Hammett; protonation pyridazine mechanism. 7145-60-0 belongs to class pyridazine, name is 6-Chloro-N,N-dimethylpyridazin-3-amine, and the molecular formula is C6H8ClN3, Application of 6-Chloro-N,N-dimethylpyridazin-3-amine.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Matsumoto, Kiyoshi published the artcileSelectivity in consecutive SNAr-dequaternization reactions of chlorodiazines with tertiary amines, Safety of 6-Chloro-N,N-dimethylpyridazin-3-amine, the main research area is dequaternization reaction chloropyrimidine tertiary amine; chloropyrimidine amination tertiary amine; dealkylation tertiary amine amination chlorodiazine; alkylmethylaminodiazine; diazine alkylmethylamino.

Consecutive SNAr-dealkylation reactions of chlorodiazines, such as, 2-chloropyrimidine (I) and 3,6-dichloropyridazine, with tertiary amines took place in a highly selective fashion. Thus, I was treated with Me2N(CH2)7Me in THF at 100° under 8 kbar pressure to give 97% 2-(methyloctylamino)pyrimidine (II) and 2% 2-(dimethylamino)pyrimidine (III).

Synthetic Communications published new progress about Amination. 7145-60-0 belongs to class pyridazine, name is 6-Chloro-N,N-dimethylpyridazin-3-amine, and the molecular formula is C6H8ClN3, Safety of 6-Chloro-N,N-dimethylpyridazin-3-amine.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Crossland, Ingolf published the artcileDimethylamination of chloropyridazines, Product Details of C6H8ClN3, the main research area is PYRIDAZINES CHLORO AMINATION.

3,6-Dichloropyridazine, 4-methyl-3,6-dichloropyridazine, the 2 trichloropyridazines, and tetrachloropyridazine are treated with aqueous Me2NH in EtOH at reflux temperature In no case is more than 1 dimethylamino group introduced, the 4- (or 5-) position being substituted in the tri- and tetra-chlorinated pyridazines. The reaction products are reductively dehalogenated and subsequently identified by N.M.R. anal. The Cl atoms ortho to the dimethylamino group are preferentially eliminated by hydrogenolysis.

Acta Chemica Scandinavica (1947-1973) published new progress about Amination. 7145-60-0 belongs to class pyridazine, name is 6-Chloro-N,N-dimethylpyridazin-3-amine, and the molecular formula is C6H8ClN3, Product Details of C6H8ClN3.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Cookson, R. F. published the artcileBasicities of pyridazine derivatives, Formula: C6H8ClN3, the main research area is Hammett basicity pyridazine; pyridazone oxygen protonation Hammett; protonation pyridazine mechanism.

The Hammett free-energy relation was used to correlate the differences in basicity of six 3-(dimethylamino)pyridazines, five 3-chloropyridazines, and seven 3-pyridazones with substituent constants; protonation occurred meta to the Me2N group of the (dimethylamino)-pyridazines, ortho to the Cl of the chloropyridazines, and on the exocyclic O of the pyridazones.

Journal of the Chemical Society, Perkin Transactions 10: Physical Organic Chemistry published new progress about Ionization. 7145-60-0 belongs to class pyridazine, name is 6-Chloro-N,N-dimethylpyridazin-3-amine, and the molecular formula is C6H8ClN3, Formula: C6H8ClN3.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Pifferi, Giorgio published the artcileSynthesis and antihypertensive properties of new 3-hydrazinopyridazine derivatives, Safety of 6-Chloro-N,N-dimethylpyridazin-3-amine, the main research area is antihypertensive hydrazinopyridazine derivative; pyridazine hydrazino derivative antihypertensive.

Of a series of 19 title compounds substituted in the 6 position with a primary or secondary amine or an alkoxy group, several were more active than hydralazine [86-54-4] in cats as hypotensive agents and as antihypertensive agents in renal hypertensive rats. I [56393-22-7] and II [56393-23-8], prepared from 3,6-dichloropyridazine [141-30-0] by displacement of 1 Cl with the appropriate amine, followed by reaction with hydrazine and benzaldehyde, followed by hydrolysis of the hydrazone, displayed high potency and low toxicity in the tests. I reduced peripheral resistance and increased aortic, femoral, and coronary blood flow in dogs. Structure-activity relations are discussed.

Journal of Medicinal Chemistry published new progress about Antihypertensives. 7145-60-0 belongs to class pyridazine, name is 6-Chloro-N,N-dimethylpyridazin-3-amine, and the molecular formula is C6H8ClN3, Safety of 6-Chloro-N,N-dimethylpyridazin-3-amine.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Matulenko, Mark A. published the artcile4-Amino-5-aryl-6-arylethynylpyrimidines: Structure-activity relationships of non-nucleoside adenosine kinase inhibitors, Synthetic Route of 17259-32-4, the main research area is aminoarylarylethynylpyrimidine derivative preparation structure adenosine kinase inhibitor analgesic pain.

A series of nonnucleoside adenosine kinase (AK) inhibitors is reported. These inhibitors originated from the modification of 5-(3-bromophenyl)-7-(6-morpholin-4-ylpyridin-3-yl)pyrido[2,3-d]pyrimidin-4-ylamine (ABT-702). The identification of a linker that would approx. the spatial arrangement found between the pyrimidine ring and the aryl group at C(7) in ABT-702 was a key element in this modification. A search of potential linkers led to the discovery of an acetylene moiety as a suitable scaffold. It was hypothesized that the aryl acetylenes, ABT-702, and adenosine bound to the active site of AK (closed form) in a similar manner with respect to the orientation of the heterocyclic base. Although potent acetylene analogs were discovered based on this assumption, an x-ray crystal structure of 5-(4-dimethylaminophenyl)-6-(6-morpholin-4-ylpyridin-3-ylethynyl)pyrimidin-4-ylamine (I) revealed a binding orientation contrary to adenosine. In addition, this compound bound tightly to a unique open conformation of AK. The structure-activity relationships and unique ligand orientation and protein conformation are discussed.

Bioorganic & Medicinal Chemistry published new progress about Analgesics. 17259-32-4 belongs to class pyridazine, name is 4-(6-Chloropyridazin-3-yl)morpholine, and the molecular formula is C8H10ClN3O, Synthetic Route of 17259-32-4.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Gokce, Mehtap published the artcileSynthesis and antinociceptive activity of 6-substituted 3-pyridazinone derivatives, Formula: C8H10ClN3O, the main research area is pyridazinone morpholino arylpiperidino arylpiperazino preparation antinociceptive activity; antinociceptive activity morpholinopyridazinone arylpiperidinopyridazinone arylpiperazinopyridazinone.

Title compounds I (X = O, CH-benzyl, N-benzyl, N-aryl) were prepared and evaluated for antinociceptive activity. In the modified Koster test in mice, I (X = NC6H4F-4) was the most active compound All the compounds except I (X = NPh) were more active than aspirin in the antinociceptive activity test.

Farmaco published new progress about Analgesics. 17259-32-4 belongs to class pyridazine, name is 4-(6-Chloropyridazin-3-yl)morpholine, and the molecular formula is C8H10ClN3O, Formula: C8H10ClN3O.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem