CAS: 7305-71-7; 2-Amino-5-Methylthiazole

上下游产品

propan-1-ol propionaldehyde thiourea 2-chloropropanal 5-methyl-1,3-thiazole-2-carbaldehyde N-(5-methylthiazol-2-yl)acetamide 4-nitro-N-5-methyl-thiazol-2-yl-benzenesulfonamide N-acetyl-sulfanilic acid-(5-methyl-thiazol-2-ylamide)N-acetyl-sulfanilic acid-(5-methyl-thiazol-2-ylamide)

异硫氰酸烯丙酯置于ammonium Hydroxide体系中,用 四氢呋喃 作为反应溶剂,化学反应 72.0H,以59%的收率获得产物2-氨基-5-甲基噻唑
参考文献:Rearrangement Reactions; 14:Synthesis Of Functionalized Thiazoles Via Attack Of Heteroatom Nucleophiles On Allenyl Isothiocyanates
标题:Rearrangement Reactions; 14:Synthesis Of Functionalized Thiazoles Via Attack Of Heteroatom Nucleophiles On Allenyl Isothiocyanates
摘要:用含硫,氧,氮或氢化物的亲核物(如丙烷-2-硫醇,噻吩酚,硫化氢,醇,酚或 Naoh,Nh3,N,N,N',N'-四甲基胍或氰基硼氢化钠等含氢化物的亲核剂,在大多数情况下会导致环闭合,反应生成在 C-2 位具有官能团的噻唑.此外,我们还首次报道了以二烷基或二苯基膦酸盐为亲核剂,通过相同策略制备芳香族噻唑-2-膦酸盐的实例.
DOI:10.1055/s-2005-872203

专利信息

专利号:US-8178672-B2
优先权日:2004-10-19
标 题:Synthesis of imidazooxazole and imidazothiazole inhibitors of p38 MAP kinase
发明人：ASHWELL MARK A; TANDON MANISH; LAPIERRE JEAN-MARC
权利人:ASHWELL MARK A; TANDON MANISH; LAPIERRE JEAN-MARC; ARQULE INC
摘要:An efficient route for the synthesis is of formula (I) of imidazooxazole and imidazothiazole inhibitors of the p38 MAP kinase pathway, useful as therapeutics for disease conditions including inflammation and auto-immune responses is described.

专利号:US-11512097-B2
优先权日:2019-11-25
标题 :Heterocyclic compounds as Delta-5 desaturase inhibitors and methods of use
发明人：ALLEN JENNIFER R; BELTRANI MICHELA; BOURBEAU MATTHEW P; DAMYANOVA TEODORA P; LINGARD IAIN; MINATTI ANA E; VINCETTI PAOLO
权利人:AMGEN INC
摘要:The present disclosure provides compounds useful for the inhibition of Delta-5 Desaturase (“D5Dâ€?). The compounds have a general Formula I n nwherein the variables of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a metabolic or cardiovascular disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.

专利号:US-5811555-A
优先权日:1995-11-22
标题:Method for substitution of an amino group of a primary amine by a chlorine atom and a synthetic method by application thereof
发明人：WAKASUGI TAKASHI; MIYAKAWA TADASHI; TANONAKA TAKAYUKI
权利人:KUREHA CHEMICAL IND CO LTD
摘要:This invention relates to methods for substitution of an amino group of a heterocyclic primary amine by a chlorine atom and synthesis of 2-chloro-5-methylthiazole and its derivatives by application thereof. n Typically, a heterocyclic primary amine and sodium nitrite are caused to react in the presence of hydrochloric acid, followed by heating the formed diazonium base at 30°-100° C. in the presence of an equimolar or more of hydrochloric acid to substitute the amino group by the chlorine atom. Further, 2-amino-5-methylthiazole and sodium nitrite are caused to react in the presence of hydrochloric acid, followed by heating the formed diazonium base at 30°-100° C. in the presence of an equimolar or over of hydrochloric acid to give 2-chloro-5-methylthiazole. Then, the resultant 2-chloro-5-methylthiazole is caused to react with a chlorinating agent to give 2-chloro-5-chloro-methylthiazole.

专利号:US-2004053999-A1
优先权日:1997-09-17
标题 :Novel compounds and methods for synthesis and therapy
发明人：BISCHOFBERGER NORBERT W; DAHL TERRENCE C; HITCHCOCK MICHAEL J M; KIM CHOUNG U; LEW WILLARD; LIU HONGTAO; MILLS ROGER G; WILLIAMS MATTHEW A
摘要:Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.

专利号:US-6225341-B1
优先权日:1995-02-27
标 题:Compounds and methods for synthesis and therapy
发明人：BISCHOFBERGER NORBERT W; KIM CHOUNG U; LEW WILLARD; LIU HONGTAO; WILLIAMS MATTHEW A
权利人:GILEAD SCIENCES INC
摘要:Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.

专利号:US-8772301-B2
优先权日:2009-12-18
标题 :Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof
发明人：HARDY LARRY WENDELL; HEFFERNAN MICHELE L R; WU FRANK XINHE; SPEAR KERRY L; SARASWAT LAKSHMI D
权利人:HARDY LARRY WENDELL; HEFFERNAN MICHELE L R; WU FRANK XINHE; SPEAR KERRY L; SARASWAT LAKSHMI D; SUNOVION PHARMACEUTICALS INC
摘要:Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.