12190-75-9Relevant articles and documents
Facile and Scalable Methodology for the Pyrrolo[2,1-f][1,2,4]triazine of Remdesivir
Roy, Sarabindu,Yadaw, Ajay,Roy, Subho,Sirasani, Gopal,Gangu, Aravind,Brown, Jack D.,Armstrong, Joseph D.,Stringham, Rodger W.,Gupton, B. Frank,Senanayake, Chris H.,Snead, David R.
, p. 82 - 90 (2022/01/28)
Pyrrolo[2,1-f][1,2,4]triazine (1) is an important regulatory starting material in the production of the antiviral drug remdesivir. Compound 1 was produced through a newly developed synthetic methodology utilizing simple building blocks such as pyrrole, chloramine, and formamidine acetate by examining the mechanistic pathway for the process optimization exercise. Triazine 1 was obtained in 55% overall yield in a two-vessel-operated process. This work describes the safety of the process, impurity profiles and control, and efforts toward the scale-up of triazine for the preparation of kilogram quantity.
Synthesis and antiproliferative assessments of new derivatives of isothiazolo[3,4-d]pyrimidine
Khoshniazi, Hamideh,Eshghi, Hossein,Tayarani-Najjaran, Mona,Tayarani-Najaran, Zahra,Saadat, Kayvan,Shiri, Ali
, p. 193 - 201 (2020/11/12)
Various derivatives of 5-aryl-4-imino-3-(phenylamino)-4,5-dihydroisothiazolo[3,4-d]pyrimidines (3a-f) were synthesized. The synthesis has been done through treatment of 3-amino-4-cyano-5-(phenylamino)isothiazole with various aryl isothiocyanates. The isothiazole skeleton was obtained by the reaction of malononitrile and phenyl isothiocyanate followed by chloramine treatment. Some of the synthesized dihydroisothiazolo[3,4-d]pyrimidines were tested against different cancer cell lines, including ACHN, HeLa, HL-60, MCF-7, and PC3. Malignant cells were cultured in RPMI medium and incubated with different concentrations of the mentioned compounds. Cell viability was assessed using the MTS assay. The cytotoxicities of the synthesized compounds are not significant and are probably safe for other biological use.
Pyrrolotriazine compounds and applications thereof
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Paragraph 0094-0098, (2020/05/01)
The invention belongs to the field of medical chemistry, and particularly relates to a class of lactam-based histone deacetylase inhibitors and a preparation method thereof, a pharmaceutical composition containing the histone deacetylase inhibitor, and applications of the inhibitors in drugs for preventing and/or treating diseases related to histone deacetylase activity out-of-control.
Discovery of a JAK1/3 Inhibitor and Use of a Prodrug to Demonstrate Efficacy in a Model of Rheumatoid Arthritis
Spergel, Steven H.,Mertzman, Michael E.,Kempson, James,Guo, Junqing,Stachura, Sylwia,Haque, Lauren,Lippy, Jonathan S.,Zhang, Rosemary F.,Galella, Michael,Pitt, Sidney,Shen, Guoxiang,Fura, Aberra,Gillooly, Kathleen,McIntyre, Kim W.,Tang, Vicky,Tokarski, John,Sack, John S.,Khan, Javed,Carter, Percy H.,Barrish, Joel C.,Nadler, Steven G.,Salter-Cid, Luisa M.,Schieven, Gary L.,Wrobleski, Stephen T.,Pitts, William J.
supporting information, p. 306 - 311 (2019/03/19)
The four members of the Janus family of nonreceptor tyrosine kinases play a significant role in immune function. The JAK family kinase inhibitor, tofacitinib 1, has been approved in the United States for use in rheumatoid arthritis (RA) patients. A number
Conjugate addition from the excited state
Iyer, Akila,Ahuja, Sapna,Jockusch, Steffen,Ugrinov, Angel,Sivaguru, Jayaraman
supporting information, p. 11021 - 11024 (2018/10/08)
Conjugate addition occurs efficiently from excited hydrazide based acrylanilides under both UV and metal free visible light irradiations. The reaction proceeds via an excited state encounter complex that bifurcates either via an electron or energy transfer pathway. The generality of excited state conjugate addition is demonstrated using chloromethylation and by thiol addition.
A simple and efficient approach to the N-amination of oxazolidinones using monochloroamine
Huynh, Uyen,Uddin, Md. Nasir,Wengryniuk, Sarah E.,McDonald, Stacey L.,Coltart, Don M.
supporting information, p. 4799 - 4802 (2016/10/05)
Chiral nonracemic N-amino cyclic carbamates (ACCs) are important auxiliaries for certain asymmetric transformations. In the past they have been synthesized from oxazolidinones using methods that require the preparation and use of non-atom economical aminating agents that can be difficult to prepare, and often strong bases. In what follows we describe a mild and operationally simple method for the direct N-amination of oxazolidinones that use NH2Cl derived from commercial bleach.
PYRROLO[2,1-F][1,2,4]TRIAZINE COMPOUND, AND PREPARATION METHOD AND APPLICATION THEREOF
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Paragraph 0021-0024, (2015/04/15)
The present invention relates to a pyrrolo[2,1-f][1,2,4]triazine compound, an isomer thereof or a pharmaceutically acceptable salt, ester or hydrate thereof, and a preparation method and application thereof. The pyrrolo[2,1-f][1,2,4]triazine compound has a structure expressed in general formula (I). The pyrrolo[2,1-f][1,2,4]triazine compound expressed in general formula (I) can inhibit a phosphatidylinositol-3 kinase (PI3K) signal pathway, thereby being used to prepare medicine for treating phosphatidylinositol-3 kinase related diseases such as cancer.
PYRROLOPYRIDAZINES AS POTASSIUM ION CHANNEL INHIBITORS
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Page/Page column 38, (2014/09/29)
A compound of formula (I) wherein A, R1, R3, and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.
AGENTS FOR TREATING NEURODEGENERATIVE DISORDERS
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Page/Page column 24, (2013/08/28)
The present invention relates to compounds of formula I, use of these compounds to treat mental and neurological disorders, especially depressions and psychoses of different etiology and methods for their preparation. The compounds provided for the treatm
NOVEL FUSED PYRIDAZINE DERIVATIVES
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Page/Page column 45-46, (2011/05/06)
The present invention relates to novel fused pyridazine compounds, their pharmaceutically acceptable salts, and their isomers, stereoisomers, conformers, tautomers, polymorphs, hydrates and solvates. The present invention also encompasses pharmaceutically acceptable compositions of said compounds and process for preparing novel compounds. The invention further relates to the use of the above-mentioned compounds for the preparation of medicament for use as pharmaceuticals.