- Pyrimidinone Derivatives as Antimalarial Agents
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The invention relates to novel pyrimidinone-based heterocyclic compounds which are parasite growth inhibitors, having the general formula (I) in which Y is a morpholine chosen from three bridged morpholines, L is a bond or a linker, n=0 or 1 and R2 is a methyl group when n=0 and a hydrogen atom when n=1. Process for the preparation thereof and therapeutic use thereof.
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- PYRIMIDINONE DERIVATIVES, PREPARATION THEREOF AND PHARMACEUTICAL USE THEREOF
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The invention relates to novel products of formula (Ia) or (Ib): these products being in all the isomeric forms and salts as drugs, notably as anticancer drugs.
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- A convenient one-pot synthesis of (R)-2-amino-3,3,3-trifluoro-2-methyl-N- phenylpropanamide derivatives
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A convenient one-pot synthesis of enantiopure (R)-2-amino-3,3,3-trifluoro- 2-methyl-N-phenylpropanamide derivatives has been developed. The key step in this synthetic methodology turned out to be the amide formation in which (R)-2-amino-3,3,3-trifluoro-2-
- Li, Tian-Wen,Shang, Pei-Hua,Cheng, Chang-Mei,Zhao, Yu-Fen
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supporting information
p. 134 - 137
(2013/02/21)
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- PYRIMIDINONE DERIVATIVES AS ANTIMALARIAL AGENTS
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The invention relates to novel pyrimidinone-based heterocyclic compounds which are parasite growth inhibitors, having the general formula (I) in which Y is a morpholine chosen from three bridged morpholines, L is a bond or a linker, n = 0 or 1 and R2 is a methyl group when n = 0 and a hydrogen atom when n = 1. Process for the preparation thereof and therapeutic use thereof.
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Page/Page column 55; 56
(2014/01/09)
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- NOVEL 2,3-DIHYDRO-1H-IMIDAZO{1,2-a}PYRIMIDIN-5-ONE and this1,2,3,4-TETRAHYDROPYRIMIDO{1,2-a}PYRIMIDIN-6-ONE DERIVATIVES COMPRISING A SUBSTITUTED MORPHOLINE, PREPARATION THEREOF AND PHARMACEUTICAL USE THEREOF
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The invention relates to the novel products of formula (I) with p, q = 0, 1 or 2; R1 = phenyl, pyridyl; -(CH2) m -Ra; alkylene; cycloalkyl; heterocycloalkyl; alkyl; -SO2 -Rb; -CO-Re; m = 1 or 2; Ra = aryl, heteroaryl, -CO-cycloalkyl, -CO-heterocycloalkyl, -CO-Rb, -C(Rb)=N-ORc, -CO 2 Rd, -CONRxRy; Rb = alkyl, aryl, heteroaryl; Rc = H, alkyl; Rd = alkyl, cycloalkyl; Re = alkyl, cycloalkyl, aryl, heteroaryl; NRxRy with Rx,Ry = H, alkyl, cycloalkyl, alkoxy, phenyl, or form with N a ring with optionally O, N; R2, R3 = H, alkyl, CF 3, or form with C a ring with optionally O, S and N; R4 = H, F, Cl, CH3 or CN; the morpholine is substituted with Me, and optionally substituted with F, OH; or is (Formula 1a) and the isomer of configuration R,R (Formula 1b) these products being in all the isomer forms and the salts, as medicaments, in particular as anticancer medicaments.
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Page/Page column 129-130
(2014/01/09)
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- NOVEL 2,3-DIHYDRO-1H-IMIDAZO(1,2-A)PYRIMIDIN-5-ONE DERIVATIVES, PREPARATION THEREOF, AND PHARMACEUTICAL USE THEREOF
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The invention relates to the novel materials of formula (I), where R1 is an optionally substituted L-aryl or -heteroaryl, such that L is: an alkyl or CO, or LX, with Lbeing an alkyl and X being O or S; R2 is H or an alkyl; R3 /
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- Convenient synthesis of N-Terminal Tfm-Dipeptides from unprotected enantiopure α-Tfm-Proline and α-Tfm-alanine
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A convenient procedure for the synthesis of highly lipophilic dipeptide building blocks from enantiopure α-trifluoromethyl α-amino acids is reported. Coupling reactions at the C termini of the trifluoromethyl a-amino acids were successfully performed with
- Chaume, Gregory,Lensen, Nathalie,Caupene, Caroline,Brigaud, Thierry
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experimental part
p. 5717 - 5724
(2010/03/01)
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- Concise synthesis of enantiopure α-trifluoromethyl alanines, diamines, and amino alcohols via the Strecker-type reaction
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Diastereomerically pure α-trifluoromethyl α-amino nitriles obtained by Strecker-type reactions from chiral CF3 imines and iminium proved to be very attractive versatile intermediates for the synthesis of various α-trifluoromethyl amino compound
- Huguenot, Florent,Brigaud, Thierry
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p. 7075 - 7078
(2007/10/03)
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