专利号:US-11325912-B2 优先权日:2019-05-09 标题 :Regio-selective synthesis of imidazo[1,2-a]pyrimidines 发明人:CLAGG KYLE BRADLEY PASCUAL; WHITE NICHOLAS ANDREW; ZHANG HAIMING; GOSSELIN FRANCIS; NACK WILLIAM; O'SHEA PAUL D 权利人:GENENTECH INC 摘要:A method of regio-selectively synthesizing an imidazo-pyrimidine compound of formulae (XXa) or (XXb)comprising a step of coupling a first compound of formula XX-P1a or XX-P1b with a second compound of formula XX-P2This annulation reaction between β-ethoxy acrylamides and phosphorylated aminoimidazoles to furnish imidazo[1,2-a]pyrimidin-amines relies on steering effects from endocyclic and exocyclic phosphorylated aminoimidazoles. The reaction furnishes either 2-amino or 4-amino constitutional isomers of imidazo[1,2-a]pyrimidines with good yields and ranges of 90:10-99:1 regio-selectivity. The reaction is useful in the synthesis of various tracer molecules used in the study of neurological conditions such as where R3 and R4 together with the imidazole ring atoms to which they are bonded form a phenyl ring and the products are substituted benzimidazopyrimidines. The reaction can be generalized to form imidazo[1,2-a]pyrimidines substituted at either of their 2- and 4-positions by alkoxy or thioalkyl groups.
专利号:US-7193039-B2 优先权日:1999-12-22 标题:Synthesis of a potent parmagnetic agonist (epm-3) of the melanocyte stimulating hormone containing amino acid-type stable free radical 发明人:NAKAIE CLOVIS RYUICHI; BARBOSA SIMONE DOS REIS; CILLI EDUARDO MAFFUD; LAMY-FREUND MARIA TEREZA; SIUITI ITO ARMANDO; VISCONTI MARIA APARECIDA; CASTRUCCI ANA MARIA DE LAURO 权利人:CONSELHO NACIONAL CNPQ 摘要:The present invention refers to the chemical synthesis and potentiality for application in several biochemical assays, of a potent agonist of the α-melanocyte stimulating hormone (α-MSH), labeled with an amino acid-type paramagnetic spin probe (Toac, or 2,2,6,6-tetramethylpiperidine-1-oxyl-amino-4-carboxylic acid), valuable for use in electron spin resonance and fluorescence allowing biochemical-clinical investigation of relevant physiological roles of α-MSH in animal organism. The referred analogue of the present invention, acetil-Toac 0 -(Nle 4 , DPhe 7 )-α-MSH, where (Nle 4 , DPhe 7 )-α-MSH is nominated commercially as Melanotanâ„¢ and although containing a non-natural compound in its structure such as Toac, maintained entirely its potent agonist potency. Its integral activity associated with the fact that it is naturally fluorescent (due to the Trp residue of its sequence) give to this labeled analogue a unique potential for a great variety of investigations regarding relevant physiological roles already known of this neuroimmuno-modulator.
专利号:US-4092329-A 优先权日:1972-12-01 标 题:Process for the synthesis of certain 2-amino-5-cyanothiophenes 发明人:JOTTERAND ARMAND 权利人:SANDOZ LTD 摘要:The invention relates to a process which comprises reacting a compound of formula I, ##STR1## in which A 1 is a radical which does not compete with the activity of the ##STR2## OR A TAUTOMER THEREOF, WITH A COMPOUND OF FORMULA II, n n a.sub.2 -- ch.sub.2 -- cn ii n n in which A 2 is a radical which does not compete with the activity of the --CH 2 CN group of the compound of formula II but provides the vicinal methylene group with sufficient acidity to react with the â•?NH group of the compound of formula I, n and with sulphur, n To obtain a compound of formula III, ##STR3## in which A 1 and A 2 are as defined above, which compounds of formula III are useful as intermediates for the production of dyestuffs.
专利号:US-8933227-B2 优先权日:2009-08-14 标题 :Selective synthesis of functionalized pyrimidines 发明人:LINZ GUENTER; KRAEMER GERD; KUSSEROW SABRINA; SCHNAUBELT JUERGEN 权利人:LINZ GUENTER; KRAEMER GERD; KUSSEROW SABRINA; SCHNAUBELT JUERGEN; BOEHRINGER INGELHEIM INT 摘要:The present invention relates to a process for making 2,4-differentiated 5-trifluoromethyl pyrimidines and 2-amino-5-trifluoromethyl-pyrimidine derivatives, which compounds are useful in the preparation of pharmacologically active compounds.
专利号:US-8981092-B2 优先权日:2008-09-19 标题 :Substituted 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-ones as modulators of protein kinase activity 发明人:MIRIZZI DANILO; CERVI GIOVANNI; D ANELLO MATTEO; PAPEO GIANLUCA MARIANO ENRICO; FERGUSON RON; CASUSCELLI FRANCESCO 权利人:MIRIZZI DANILO; CERVI GIOVANNI; D ANELLO MATTEO; PAPEO GIANLUCA MARIANO ENRICO; FERGUSON RON; CASUSCELLI FRANCESCO; NERVIANO MEDICAL SCIENCES SRL 摘要:Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds, n nor pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.
专利号:US-6479668-B1 优先权日:1998-09-08 标 题 :Method of producing pyrrolidine derivatives 发明人:MURAOKA HIDEO; SATO HARUYO 权利人:TORAY INDUSTRIES 摘要:A method for producing pyrrolidine derivatives such as 3,4-epoxypyrrolodines, 3-pyrrolidols and the like, by oxidizing 3-pyrrolines with at least one peroxide in the presence of at least one acid is disclosed. The 3-pyrrolines are produced by deriving cis-2-butene compounds from cis-2-butene-1,4-diols and performing a cyclization between the cis-2-butene derivatives and at least one primary amine. The method may be performed as a one-pot synthesis and may be performed as a continuous reaction.
参考标题:Efficient Synthesis Of N-Sulfonylacetamidines From Propiolic Acid By Copper-Catalyzed Three-Component Coupling Reactions 作者:Chunxiang Kuang,Qing Yang,Mei Xu,Zhuo Wang |发布日期:2010.10 摘要:Using Propiolic Acid As One Of The Reacting Components, A Copper-Catalyzed Three-Component Reaction Of Sulfonyl Azide And Amines Affords N-Sulfonylacetamidines Via A Decarboxylation Process In High Yields Under Mild Conditions. This One-Pot Method Is Efficient, General, And Versatile.
合成参考文献
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