{"id":11933,"date":"2023-01-04T08:11:31","date_gmt":"2023-01-04T00:11:31","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=11933"},"modified":"2023-01-04T08:11:31","modified_gmt":"2023-01-04T00:11:31","slug":"alberti-carlo-et-al-published-their-research-in-farmaco-edizione-scientifica-in-1967-cas-14678-93-4","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=11933","title":{"rendered":"Alberti, Carlo et al. published their research in Farmaco, Edizione Scientifica in 1967 | CAS: 14678-93-4"},"content":{"rendered":"<p>Sulfanilamidopyrazoles.  IX.  Chloro, methyl, and methoxy derivatives of 1-phenyl-5-sulfanilamidopyrazole was written by Alberti, Carlo;Tironi, C.. And the article was included in Farmaco, Edizione Scientifica in 1967.<a href=\"https:\/\/www.ambeed.com\/products\/14678-93-4.html\">Application of 14678-93-4<\/a> This article mentions the following:<\/p>\n<p>Pyrazoles of the general formula I are prepared; the introduction of Cl, Me, or MeO into the 1-phenyl ring decreases the bacteriostatic activity of I (R = X = H, Ar = p-H2NC6H4SO2) against Staphylococcus aureus and Escherichia coli. Thus, 2.9 g. o-ClC6H4NHNH2 in 10 ml. EtOH is treated with 3.4 g. EtOCH:C(CO2Et)CN in 10 ml. EtOH to give 65% Et \u03b1-cyano-\u03b2-[2-(o-chlorophenyl)hydrazino]acrylate (II), m. 147-8\u00b0 (EtOH). Similarly prepared are (m.p. and % yield given): o-MeC6H4NHNHCH:C(CO2Et)CN, 147-8\u00b0 (C6H6), 90; o-MeOC6H4NHNHCH:C(CO2Et)CN, 118-19\u00b0 (C6H6), 61. A solution of 5.3 g. II in 50 ml. HOAc is refluxed 3 hrs. to give 80% Et 5-amino-1-(o-chlorophenyl)pyrazole-4-carboxylate, m. 83-4\u00b0 (C6H6). Similarly prepared are (m.p. given): I (Ar = H, X = o-Me, R = CO2Et), 58-9\u00b0 (EtOH-water); I (Ar = H, X = o-MeO, R = CO2Et), 78-9\u00b0 (ligroine). A solution of 16.9 g. EtOCH:C(CO2Et)CN and 14.25 g. m-ClC6H4NHNH2 in 100 ml. EtOH is refluxed 3 hrs. to give 96% I (Ar = H, X = m-Cl, R = CO2Et), m. 117-18\u00b0 (EtOH). Similarly prepared are the following I (Ar = H, R = CO2Et) (X and m.p. given): p-Cl, 148-9\u00b0 (EtOH); m-Me, 65-6\u00b0 (C6H6); p-Me, 114-15\u00b0 (C6H6); m-MeO, 71-2\u00b0 (ligroine); p-MeO, 110-11\u00b0 (ligroine). The I (R = CO2Et) are heated with 2N NaOH to give the following I (Ar = H, R = CO2H) (X and m.p. given): o-Cl, 170-1\u00b0; m-Cl, 152-3\u00b0; p-Cl, 192-3\u00b0; o-Me, 167-8\u00b0; m-Me, 169-70\u00b0; p-Me, 178-9\u00b0; o-MeO, 154-5\u00b0; m-MeO, 166-7\u00b0; p-MeO, 184-5\u00b0. I (Ar = H, R = CO2H, X = o-Me) (4.4 g.) is heated at 170-80\u00b0 to give 95% 1-(o-tolyl)-5-aminopyrazole, m. 57-8\u00b0 (C6H6). Similarly prepared are the following I (Ar = R = H) (X and m.p. given): p-Me, 53-4\u00b0 (ligroine); o-MeO, [HCl salt m. 216-17\u00b0 (EtOH-Et2O)]; m-MeO, 65-6\u00b0; p-MeO, 87-8\u00b0. A mixture of 4.75 g. I (Ar = H, R = CO2H, X = o-Cl) and 70 ml. 75% H2SO4 is heated at 150-60\u00b0 to give 78% I (Ar = R = H, X = o-Cl) (III), m. 56-7\u00b0 (ligroine-ether); HOAc can also be used. Similarly prepared are the following I (Ar = R = H) (X and m.p. given): m-Cl, 91-2\u00b0; p-Cl, 82-3\u00b0 (ligroine); m-Me, [HCl salt m. 217-18\u00b0 (EtOH-Et2O)]. A mixture of 3.8 g. III, 4.7 g. p-AcNHC6H4SO2Cl, and 10 ml. pyridine is heated 15 min. at 40-50\u00b0 and kept 12 hrs. at room temperature to give 90% 1-(o-chlorophenyl)-5-(p-acetamidobenzenesulfonamido)pyrazole (IV), m. 238-9\u00b0 (dilute EtOH). Similarly prepared are the following I (Ar = p-AcNHC6H4SO2, R = H) (X and m.p. given): p-Cl, 244-5\u00b0; o-Me, 237-8\u00b0; m-Me, 209-10\u00b0; p-Me, 257-8\u00b0; o-MeO, 210-11\u00b0; m-MeO, 181-2\u00b0; p-MeO, 230-1\u00b0. A mixture of 3.9 g. IV and 40 ml. 5% NaOH is refluxed to give 87% 1-(o-chlorophenyl)-5-sulfanilamidopyrazole, m. 145-6\u00b0. Similarly prepared are the following I (Ar = p-H2NC6H4SO2, R = H) (X and m.p. given): m-Cl, 139-40\u00b0; p-Cl, 164-5\u00b0; o-Me, 166-7\u00b0; m-Me, 123-4\u00b0; p-Me, 161-2\u00b0; o-MeO, 161-2\u00b0; m-MeO, 178-9\u00b0; p-MeO, 162-3\u00b0. Phenylhydrazines are treated with mixtures of Ac2O and acrylonitrile, N1-phenyl-N2-(2-cyanoethyl)hydrazines are not obtained; the following compounds are isolated (m.p. given): o-ClC6H4NHNHAc, 119-20\u00b0; m-ClC6H4NHNHAc, 133-4\u00b0; p-ClC6H4NHNHAc, 156-7\u00b0. In the experiment, the researchers used many compounds, for example, 5-Amino-1-(p-tolyl)-1H-pyrazole-4-carboxylic acid (cas: 14678-93-4<a href=\"https:\/\/www.ambeed.com\/products\/14678-93-4.html\">Application of 14678-93-4<\/a>).<\/p>\n<p>5-Amino-1-(p-tolyl)-1H-pyrazole-4-carboxylic acid (cas: 14678-93-4) belongs to pyrazole derivatives. An alternative way to synthesize multisubstituted pyrazoles is the Csingle bondH arylation of simple pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, antidiabetic and antibacterial activities.<a href=\"https:\/\/www.ambeed.com\/products\/14678-93-4.html\">Application of 14678-93-4<\/a><\/p>\n<p>Referemce:<br \/><a href=\"https:\/\/en.wikipedia.org\/wiki\/Pyrazole\">Pyrazole &#8211; Wikipedia<\/a>,<br \/><a href=\"https:\/\/www.sciencedirect.com\/topics\/chemistry\/pyrazoles\">Pyrazoles &#8211; an overview | ScienceDirect Topics<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"<p>5-Amino-1-(p-tolyl)-1H-pyrazole-4-carboxylic acid (cas: 14678-93-4) belongs to pyrazole derivatives. An alternative way to synthesize multisubstituted pyrazoles is the Csingle bondH arylation of simple pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, antidiabetic and antibacterial activities.<a href=\"https:\/\/www.ambeed.com\/products\/14678-93-4.html\">Application of 14678-93-4<\/a><\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[131],"tags":[129],"class_list":["post-11933","post","type-post","status-publish","format-standard","hentry","category-pyrazoles-derivatives","tag-200-300"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v24.9 - https:\/\/yoast.com\/wordpress\/plugins\/seo\/ -->\n<title>Alberti, Carlo et al. published their research in Farmaco, Edizione Scientifica in 1967 | CAS: 14678-93-4 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Sulfanilamidopyrazoles. 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