- One-pot synthesis of stable phosphorus ylides by three-component reaction between arylglyoxals, phosphines and barbituric or Meldrum’s acid
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An efficient one-pot method for the synthesis of new substituted phosphorus ylides is described via three-component reaction between arylglyoxals, C–H acids such as barbituric acid and Meldrum’s acid and triphenylphosphine or tri-n-octylphosphine. This re
- Latifi, Mahsa,Anary-Abbasinejad, Mohammad
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p. 133 - 139
(2022/01/28)
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- Development of an efficient, scalable route for the preparation of a novel insulin-like growth factor-1 receptor modulator
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A chromatography-free and efficient synthesis of insulin-like growth factor-1 receptor (IGF-1R) modulator is reported. Herein we describe an improved synthesis for the target compound, which features facile introduction of a novel pyrrolidinyl-pyrimidyl isoxazole 8, via in situ sulfone displacement by fluorine. The overall process consists of six chemical steps and five isolations, with introduction of the expensive triheterocyclic unit 8 towards the end of the synthesis.
- Kumar, C.H. Vinod,Kavitake, Santosh,Kumar, Sythana Suresh,Cornwall, Philip,Ashok, Mithun,Bhagat, Sagar,Manjunatha, Sulur G.,Nambiar, Sudhir
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p. 1416 - 1421
(2012/10/29)
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- NITROGENATED FUSED RING DERIVATIVE, PHARMACEUTICAL COMPOSITION COMPRISING THE SAME, AND USE OF THE SAME FOR MEDICAL PURPOSES
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[Purpose] The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like. [Solution] The present invention provides nitrogen-containing fused ring derivatives represented by the following general formula (I) which has a GnRH antagonistic activity, prodrugs, salts, pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A and B are independently aryl or heteroaryl; RA and RB are independently halogen, cyano, alkyl, alkylsulfonyl, -OW1, -SW1, -COW2, -NW3W4, -SO2NW3W4, aryl, etc.; RC is H or alkyl; E is oxygen atom, etc.; U is single bond or alkylene; and X is Y, -CO-Y, -SO2-Y -S-(alkylene)-Y, -O-(alkylene)-Y, -SO2-(alkylene)-Y, etc.; Y is Z or amino, etc.; and Z is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, etc.
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Page/Page column 45
(2010/01/29)
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- S-6-METH0XY-2- (2- (3- (PYRIMID-2-YL) IS0XAZ0L-5-YL) PYRROLIDIN-1-YL) -4- (5-METHYL-IH-PYRAZOL-S-YLAMINO) PYRIMIDINE AND POLYMORPHIC FORMS THEREOF AS MODULATORS OF THE INSULIN-LIKE GROWTH
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There is provided novel pyrimidine derivatives of formula (I) or pharmaceutically acceptable salsts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
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Page/Page column 29
(2008/12/04)
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- PYRIMIDINE DERIVATIVES FOR THE INHIBITION OF IGF-IR TYROSINE KINASE ACTIVITY
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A compound of formula (I) wherein the substituents are as defined in the text for use in inhibiting insulin-like growth factor 1 receptor activity in a warm blooded animal such as man.
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Page/Page column 96
(2008/06/13)
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- 4-(PYRID-2-YL) AMINO SUBSTITUTED PYRIMIDINE AS PROTEIN KINASE INHIBITORS
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A compound of formula (I): wherein the substituents are as defined in the text for use in inhibiting insulin-like growth factor 1 receptor activity in a warm-blooded animal such as man.
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Page/Page column 97
(2008/06/13)
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- ALKYLATION OF BARBITURIC ACIDS BY ALCOHOLS AS A METHOD FOR THE SYNTHESIS OF 6-ALKOXYURACILS
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The alkylation of barbituric acid, 2-thiobarbituric acid, and their N-methyl derivatives by aliphatic alcohols in the presence of acidic catalysts gives high yields of 6-alkoxyuracils.In the case of methanol and 2-methyl-1-propanol the best catalyst is boron trifluoride etherate. 2-Thiobarbituric acids are alkylated more easily than the corresponding barbituric acids.
- Rudenko, E. S.,Krasnov, K. A.,Slesarev, V. I.
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p. 2337 - 2341
(2007/10/02)
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- REACTION OF BARBITURIC ACID AND ITS METHYL DERIVATIVES WITH DIAZOMETHAN IN ETHERS
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A full scheme for the methylation of barbituric acid with diazomethane in diethyl ether, glyme, and THF was formulated.For barbituric acid and its N-methyl derivatives the reaction takes place at the oxygen atoms of the β-dicarbonyl fragment.The 6-methoxyuracil and its derivatives which are formed here are subsequently methylated at the nitrogen and oxygen atoms.The reaction takes place in accordance with the structures of the monoanions of the compounds being methylated.
- Krasnov, K. A.,Slesareva, V. I.,Studentsov, E. P.,Slesarev, V. I.
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p. 1765 - 1769
(2007/10/02)
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- SOLVATION EFFECTS IN THE METHYLATION OF BARBITURIC ACID AND ITS DERIVATIVES BY DIAZOMETHANE
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Methylation of barbituric acid and its N-methylderivatives by diazomethane in ethers and methanol occurs only at the oxygen atom of the β-dicarbonyl fragment.The resulting 6-methoxy-2,4-dioxo-1,2,3,4-tetrahydropyrimidine and its derivatives are methylated at both the oxygen and nitrogen atoms; relative to ethers, methanol facilitates a greater degree of methylation at the nitrogen atom.
- Krasnov, K. A.,Slesarev, V. I.,Zakharov, A.P.,Grigor'eva, E. G.
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p. 1218 - 1221
(2007/10/02)
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