- Preparation of pyrrole and pyrrolidine derivatives of pyrimidine. 1-(2-Pyrimidinyl)pyrrole - An inhibitor of X. Phaseoli and X. Malvacearum
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Pyrrole and pyrrolidine derivatives of pyrimidine were prepared in which the nitrogen atom of the pyrrole or pyrrolidine ring is bonded directly to the 2- or 4-carbon atom of the pyrimidine ring. Pyrrole derivatives were prepared by the dry distillation of an intimate mixture of an aminopyrimidine with mucic acid and by the reaction of a chloropyrimidine with potassium pyrrole. Pyrrolidine derivatives were prepared by the reaction of a chloropyrimidine with pyrrolidine and, in a single instance, by the catalytic hydrogenation of a pyrimidinylpyrrole. At a concentration of 200 mcg/mL, 1-(2-pyrimidinyl)pyrrole inhibited two plant pathogenic bacteria -Xanthomanus phaseoli (pathogenic on the bean plant) and Xanthomanus malvacearum (pathogenic on the cotton plant).
- Becker, Irwin
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- Zero-wastewater preparation method of 2-amino-4-methylpyrimidine compound
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The invention discloses a zero-wastewater preparation method of a 2-amino-4-methylpyrimidine compound. 4,4-dimethoxy-2-butanone reacts with guanidine hydrochloride under an alkali condition, and simple post-treatment is carried out to obtain the product. No process wastewater is generated, so that the problem that a large amount of wastewater is generated in current production is solved. The operation process is simple and stable, the safety is high, the energy consumption is low, and industrial implementation is easy.
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Paragraph 0023-0024
(2020/05/02)
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- MECHANISTIC TARGET OF RAPAMYCIN SIGNALING PATHWAY INHIBITORS AND THERAPEUTIC APPLICATIONS THEREOF
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Selective mTOR inhibitors of formulas (I)-(III), processes for their preparation, pharmaceutical compositions containing them, and their use in the treatment of diseases and disorders, arising from abnormal cell growth, functions, or behaviors mediated by an mTOR kinase and/or one or more PI3K enzyme, are provided. Such diseases and disorder include cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
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Paragraph 00187; 00188
(2018/04/11)
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- Identification of NVP-BKM120 as a potent, selective, orally bioavailable class i PI3 kinase inhibitor for treating cancer
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Phosphoinositide-3-kinases (PI3Ks) are important oncology targets due to the deregulation of this signaling pathway in a wide variety of human cancers. Herein we describe the structure guided optimization of a series of 2-morpholino, 4-substituted, 6-heterocyclic pyrimidines where the pharmacokinetic properties were improved by modulating the electronics of the 6-position heterocycle, and the overall druglike properties were fine-tuned further by modification of the 4-position substituent. The resulting 2,4-bismorpholino 6-heterocyclic pyrimidines are potent class I PI3K inhibitors showing mechanism modulation in PI3K dependent cell lines and in vivo efficacy in tumor xenograft models with PI3K pathway deregulation (A2780 ovarian and U87MG glioma). These efforts culminated in the discovery of 15 (NVP-BKM120), currently in Phase II clinical trials for the treatment of cancer.
- Burger, Matthew T.,Pecchi, Sabina,Wagman, Allan,Ni, Zhi-Jie,Knapp, Mark,Hendrickson, Thomas,Atallah, Gordana,Pfister, Keith,Zhang, Yanchen,Bartulis, Sarah,Frazier, Kelly,Ng, Simon,Smith, Aaron,Verhagen, Joelle,Haznedar, Joshua,Huh, Kay,Iwanowicz, Ed,Xin, Xiaohua,Menezes, Daniel,Merritt, Hanne,Lee, Isabelle,Wiesmann, Marion,Kaufman, Susan,Crawford, Kenneth,Chin, Michael,Bussiere, Dirksen,Shoemaker, Kevin,Zaror, Isabel,Maira, Sauveur-Michel,Voliva, Charles F.
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supporting information; experimental part
p. 774 - 779
(2011/12/03)
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- SUBSTANCES FOR DYEING KERATINOUS FIBERS
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Disclosed are substances which contain unsaturated, non-aromatic dialdehydes of formula (Ia) and/or the tautomer (Ib) thereof, wherein R1, R2, and R3 are defined as indicated in claim 1, along with at least one CH-acidic compound of formulas (II) and/or (III), wherein R6, R7, R8, R9, R10, Y, X?, Het, and X1 are defined as indicated in claim 1, in a cosmetic carrier. Said substances color keratinous fibers, especially human hair, in an intensive, colorfast, natural brown shade.
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- PYRIMIDINE DERIVATIVES USED AS PI-3 KINASE INHIBITORS
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Phosphatidylinositol (PI) 3-kinase inhibitor compounds (I), their pharmaceutically acceptable salts, and prodrugs thereof ; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases.
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Page/Page column 92-93
(2010/11/28)
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- Highly efficient synthesis of pyrimidines under microwave-assisted conditions
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Microwave irradiation of an amidine and alkynone in acetonitrile at 120°C gives 2,4-disubstituted and 2,4,6-trisubstituted pyrimidines in very high yield.
- Bagley, Mark C.,Hughes, David D.,Taylor, Paul H.
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p. 259 - 261
(2007/10/03)
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- SUBSTITUTED QUINAZOLINE DERIVATIVES AND THEIR USE AS INHIBITORS
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The use of a compound of formula (I) 1 or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2, or NR6 where R6 is hydrogen or C1-6 alkyl,; R5 is an optionally substituted 5-membered heteroaromatic ring, R1, R2 ,R3, R4 are independently selected from various specified moieties, in the preparation of a medicament for use in the inhibition of aurora 2 kinase. Certain compounds are novel and these, together with pharmaceutical compositions containing them are also described and claimed
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- Preparation of 4-methylpyrimidines
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A process for the preparation of a 4-methylpyrimidine of the general formula I STR1 in which R1 denotes C1 -C20 alkyl, C3 -C8 cycloalkyl, aryl, C7 -C12 phenalkyl, C7 -C12 alkylphenyl, NH2, NHCN, OH, and SH, in which a 1-aminovinyl methyl ketone of the general formula II STR2 in which R2 and R3 denote C1 -C20 alkyl, C3 -C8 cycloalkyl, aryl, C7 -C12 phenylalkyl, C7 -C12 alkylphenyl, C1 -C20 hydroxyalkyl or together denote a C2 -C7 alkylene chain optionally mono- to tetra-substituted by C1 -C4 alkyl and optionally interrupted by oxygen, nitrogen, or sulfur, is caused to react with a carboxamide or amidine or a salt thereof of the general formula III STR3 in which R1 has the aforementioned meanings and x stands for oxygen or NH, at temperatures ranging from 20° to 200° C. and pressures ranging from 0.01 to 50 bar.
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- Reaction of 2-Dimethylaminomethylene-1,3-diones with Dinucleophiles. VIII. Synthesis of Ethyl and Methyl 2,4-Disubstituted 5-Pyrimidinecarboxylates
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Reaction of ethyl or methyl 2-dimethylaminomethylene-3-oxoalkanoates with N-C-N dinucleophiles such as guanidine, acetamidine or benzamidine afforded in high yields the relative esters of 4-substituted 2-amino-, 2-methyl- or 2-phenyl-5-pyrimidinecarboxylic acids, respectively.These esters were hydrolyzed to the corresponding carboxylic acids, which were converted by heating to 4-substituted 2-pyrimidinamines, 2-methyl or 2-phenylpyrimidines, respectively, generally in excellent yields.The 4-unsubstituted ethyl 2-amino-, 2-methyl- and 2-phenyl-5-pyrimidinecarboxylateswere obtained in moderate yields by reaction of the above dinucleophiles with ethyl 2,2-diformylacetate.These esters were hydrolyzed and the corresponding acids (with the exception of the 2-methyl derivative) were decarboxylated to give 2-pyrimidinamine and 2-phenylpyrimidine in satisfactory yields.
- Schenone, Pietro,Sansebastiano, Laura,Mosti, Luisa
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p. 295 - 305
(2007/10/02)
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