- Simple 2-amino-5-halogenated pyridine preparation method
-
The invention provides a 2-amino-5-halogenated pyridine preparation method, which comprises: carrying out an addition reaction on 4-cyano-1-butyne and a halogen element X2 in a solvent under the catalysis of an acidic catalyst to obtain 4,4,5,5-tetrahalogenated n-valeronitrile, and carrying out cyclization on the 4,4,5,5-tetrahalogenated n-valeronitrile and ammonia through pyridine to obtain 2-amino-5-halogenated pyridine. According to the present invention, the preparation method has advantages of mild preparation condition, safety, environmental protection, low cost, high selectivity, less by-products and high product yield, and is suitable for industrial production.
- -
-
Paragraph 0037-0040
(2019/10/01)
-
- Triazole methyl ester linked spiro compound with antibacterial activity, and preparation method and application thereof
-
The invention discloses a triazole methyl ester linked spiro compound with antibacterial activity, and a preparation method and application thereof, and belongs to the technical field of medicine synthesis. The key point of the technical scheme is as follows: the triazole methyl ester linked spiro compound with antibacterial activity has the following structure: (the formula is shown in the description). The invention also discloses a preparation method of the triazole methyl ester linked spiro compound with antibacterial activity. The reaction process is simple and practical in operation, theraw materials are cheap and easily available, the reaction efficiency is high, the repeatability is high, and a remarkable inhibition effect on escherichia coli is achieved.
- -
-
-
- NOVEL TRICYCLIC COMPOUNDS AS INHIBITORS OF MUTANT IDH ENZYMES
-
The present invention is directed to tricyclic compounds of formula (I), (Ia) or (Ib) which are inhibitors of one or more mutant IDH enzymes. The present invention is also directed to uses of these tricyclic compounds in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
- -
-
Page/Page column 44; 45
(2017/05/17)
-
- PROCESS FOR THE CATALYTIC DIRECTED CLEAVAGE OF AMIDE-CONTAINING COMPOUNDS
-
The present invention relates to a catalytic method for the conversion of amide-containing compouds by means of a build-in directing group and upon the action of a heteronucleophilic compound (in se an amine (RNH2 or RNHR') or an alcohol (ROH) or a thiol (RSH)) in the presence of a metal catalyst to respectively esters, thioesters, carbonates, thiocarbonates and to what is defined as amide-containing compounds (such as carboxamides, urea, carbamates, thiocarbamates). The present invention also relates to these amide-containing compounds having a build-in directing group (DG), as well as the use of such directing groups in the catalytic directed cleavage of N-DG amides with the use of heteronucleophiles (in se an amine (RNH2 or RNHR') or an alcohol (ROH) or thiol (RSH)).
- -
-
Page/Page column 51; 53
(2017/04/11)
-
- Synthesis and pharmacological evaluation of a second generation of pyridothiadiazine 1,1-dioxides acting as AMPA potentiators
-
Taking into account structure-activity relationships obtained with our previous series, new diversely substituted 1,2,4-pyridothiadiazine 1,1-dioxides were designed to obtain novel AMPA potentiators. The aim of this work was focused on the improvement of lipophilicity, which is well known as a critical parameter to obtain in vivo active central nervous system agents. For this purpose, two positions on the pyridine ring were privileged to insert selected groups. Among the synthesized compounds emerged 7-chloro-4-ethyl-3,4-dihydro-2H-pyrido[2,3-e]-[1,2,4]-thiadiazine 1,1-dioxide (12d), which was evaluated in two memory tests in Wistar rats and showed cognition enhancing effects after intraperitoneal injection at doses as low as 0.3 mg/kg.
- Francotte, Pierre,Tullio, Pascal de,Podona, Tchao,Diouf, Ousmane,Fraikin, Pierre,Lestage, Pierre,Danober, Laurence,Thomas, Jean-Yves,Caignard, Daniel-Henri,Pirotte, Bernard
-
scheme or table
p. 9948 - 9956
(2009/04/05)
-