885-12-1Relevant articles and documents
Synthesis method of remdesivir intermediate triazinamine derivative
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, (2021/04/10)
The invention discloses a synthesis method of a remdesivir intermediate triazinamine derivative. The remdesivir intermediate triazinamine derivative is prepared by adopting a unique synthesis method. The invention solves the problems of expensive raw materials, large amount of wastewater in the production process and the like in existing reaction of a remdesivir intermediate triazinamine derivative, and provides the novel synthesis method of the remdesivir intermediate triazinamine derivative, wherein the synthesis method has the advantages of simple preparation method, cheap and easily available raw materials, greatly reduced production cost, less wastewater and the like; the synthesis method is never reported in the prior art, is a brand-new preparation method of the remdesivir intermediate triazinamine derivative, and provides a new synthesis idea for similar compounds of remdesivir.
Synthesis method of key intermediate 7-halogenated pyrrolo[1,2-F][1,2,4]triazin-4-amine of remdesivir
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, (2021/08/14)
The invention discloses a synthesis method of a key intermediate 7-halogenated pyrrolo[1,2-F][1,2,4]triazin-4-amine of remdesivir as shown in a formula (h). Phthalimide is used as a raw material, and the key intermediate 7-halogenated pyrrolo[1,2-F][1,2,4]triazin-4-amine of remdesivir is synthesized through a series of reactions such as substitution, cyclization, bromination, cyano substitution, hydrazinolysis, heterocyclic ring synthesis and iodination . The post-treatment operation is optimized, and the method has the advantages of being short in reaction time, high in yield, suitable for industrial production and the like.
HETEROCYCLIC COMPOUNDS
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Page/Page column 83, (2018/07/29)
The present invention relates to compounds of the general formula (1) wherein the variables are defined as given in the description and claims. The invention further relates to uses of and to, processes and intermediates related to compounds of the general formula (I), wherein Q is wherein the substituents of I, Ia and Ib are as defined in description and claims.
PYRROLOPYRIDAZINE JAK3 INHIBITORS AND THEIR USE FOR THE TREATMENT OF INFLAMMATORY AND AUTOIMMUNE DISEASES
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Page/Page column 62, (2012/10/07)
Disclosed are compounds of formula (I) and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.
PYRROLOPYRIDAZINE JAK3 INHIBITORS AND THEIR USE FOR THE TREATMENT OF INFLAMMATORY AND AUTOIMMUNE DISEASES
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Page/Page column 73, (2012/10/07)
Disclosed are compounds of Formula (I), and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.
HETEROCYCLIC COMPOUND AS PROTEIN KINASE INHIBITOR
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, (2011/08/06)
Provided are novel heterocyclic compounds useful as anti-cancer drugs by suppressing protein kinase activities of growth factor receptors such as c-Met, pharmaceutical compositions containing the same, and methods for using the compound.
1,1′-Bipyrroles: Synthesis and stereochemistry
Dey, Sanjeev K.,Lightner, David A.
, p. 9395 - 9397 (2008/03/13)
(Chemical Equation Presented) 1,1′-Bipyrrole is synthesized in four steps from hydrazine. A colorless solid, mp 52°C, it sublimes readily at room temperature and forms X-ray quality crystals in which the rings are not coplanar but are nearly orthogonal.
Tautomerism in the solid state and in solution of a series of 6-aminofulvene-1-aldimines
Sanz, Dionisia,Perez-Torralba, Marta,Alarcon, Sergio Hugo,Claramunt, Rosa Maria,Foces-Foces, Concepcion,Elguero, Jose
, p. 1462 - 1471 (2007/10/03)
To study systems able to sustain intramolecular proton-transfer, we have prepared a series of six aminofulvene aldimines including several labeled with 15N and 2H. These compounds show coupling constants through the hydrogen bond, 1hJ(15N-1H) and 2hJ(15N-15N). The position of the tautomeric equilibria, i.e., on what nitrogen atom is the proton, was determined in the solid state and in solution. The crystal structure of N{([5-[(phenylamino)methylene]- 1,3-cyclopentadien-1-yl]methylene})pyrrole-1-amine (3) has been determined by X-ray analysis. In solution, both N-H and C-H tautomers were observed and their structures assigned by NMR spectroscopy. Particularly useful is the value of the 1J(15N-1H) coupling constant.
3-substituted cephem compounds
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, (2008/06/13)
The present invention relates to novel cephalosporins of the formula (I); STR1 wherein, R1 represents a C1 ?C4 alkyl group or STR2 wherein, R2 and R3, independently, represent hydrogen or a C1 ?C3 alkyl group and R4 represents hydrogen or a C1 ?C4 alkyl group; R1a represents hydrogen or an amino-protecting group; Q represents CH or N; and the formula STR3 represents a saturated or unsaturated heterocyclic group which contains 1 to 4 nitrogen atoms of which one is substituted with an amino group to form quaternary ammonium, and oxygen or sulfur, or a fused heterocyclic group thereof formed together with a substituted or unsubstituted benzene or an optional heterocyclic group, or a pharmaceutically acceptable salt thereof, to processes for preparing the same and to a pharmaceutical composition containing the same as an active ingredient. The compounds(1) according to the invention exhibit potent antibacterial activity and broad antibacterial spectrum against the Gram-positive strains including Staphylococcus as well as Gram-negative strains including Pseudomonas, and, therefore, are expected to be very useful in treatment of various diseases caused by bacterial infection in human beings and animals.
A NOVEL SYNTHESIS OF PYRROMETHENONES
Jacobi, Peter A.,Buddhu, Subhas C.
, p. 4823 - 4826 (2007/10/02)
Pyrromethenones are prepared by a process involving acylation of an N-aminopyrrole with a suitable acetylenic acid, followed by sequential 5-exo-dig cyclization and 3,5-sigmatropic shift.