220882-43-9

Upstream product

• 151917-39-4 ethyl 6-iodonicotinate 
• 1066-54-2 trimethylsilylacetylene 
• 132334-98-6 ethyl 6-bromopyridine-3-carboxylate 
• 49608-01-7 6-chloro-3-pyridinecarboxylic acid ethyl ester 
• 622374-63-4 6-[(3-methyl-3-hydroxy)but-1-yn]nicotinic acid ethyl ester 
• 216443-99-1 ethyl 6-trimethylsilylethynyl-3-pyridine-carboxylate 

Downstream Products

• 1029358-83-5 ethyl 6-(6-[4-(2-trifluoromethylbenzoyl)piperazin-1-yl]-pyridin-3-ylethynyl)nicotinate 

Relevant academic research and scientific papers

GOLD (I)-PHOSPHINE 1,2,3-TRIAZOLE DERIVATIVES WITH ANTIOBIOTIC PROPERTIES

The present invention relates to gold (l)-phosphine 1,2,3-triazole compounds, and their use in a human or animal medicine. The present invention also relates to using such compounds for the prevention and/or treatment of an infection, i.e. inhibitors of growth of Gram-positive and/or Gram-negative bacteria. On another aspect the invention relates to the synthesis of the gold (l)-phosphine compounds of the invention and to their synthesis intermediates. The present invention finds applications in the medical, veterinary and/or chemical fields.

INHIBITORS OF COLLAGEN PROLYL 4-HYDROXYLASE

Biheteroaryl dicarboxylates and esters, and salts thereof which are useful as modulators of CP4H activity and more particularly as inhibitors of CP4H. Compounds of formula: and salts thereof where: X is S, O, NH, or NR, where R is an alkyl group having 1-3 carbon atoms; R1 and R2 independently are —OR7, or —NHSO2R8, where R7 is selected from: hydrogen, alkyl, alkenyl, alkoxyalkyl, —R′—CO—R″, —R′—CO—O—R″, —CO—R″, —R′—O—CO—R″, —R′—CO—NR″, —CO—NR″, or —R′—O—CO—NR″, and R8 is selected from hydrogen, alkyl, aryl, arylalkyl; R3, R4 and R6 independently are hydrogen, alkyl, alkoxy, alkenyl, alkenoxy, halo alkyl, haloalkenyl, halogen, hydroxyl, hydroxyalkyl, hydroxyalkenyl, aryl, aryloxy, arylalkyl or arylalkyloxy; R5 is hydrogen, halogen, alkyl having 1-3 carbon atoms, or alkoxy having 1-3 carbon atoms; —R′— is a divalent straight chain or branched alkylene, and —R″ is an alkyl, alkenyl, arylalkyl, or aryl group. Methods for inhibition of CP4H in vivo and in vitro.

A process for the preparation of tazarotene

Tazarotene is prepared by deoxygenation of the corresponding S-oxide, in turn obtained according to two alternative synthetic pathways.

Process for the preparation of Tazarotene

Tazarotene is prepared by deoxygenation of the corresponding S-oxide, in turn obtained according to two alternative synthetic pathways.

A practical and efficient process for the preparation of tazarotene

We describe an efficient process for the preparation of tazarotene starting from 4,4-dimethyl-6-bromothiochromane S-oxide (9), 2-methyl-3-butyn-2-ol (10), and 6-chloronicotinic acid ethyl ester (8). Our synthetic pathway compares favorably over the previously reported procedures since tazarotene was prepared straightforwardly using cheap reagents and without the employment of hazardous organometallic compounds. The process is based on the use of sulfoxide 9 as key starting material. The C-15 framework of the target was built up by means of two different approaches based on a palladium-mediated coupling reaction. The molecular structure of compound has been confirmed by X-ray crystallography.

NOVEL LIGANDS THAT ARE ANTAGONISTS OF RAF RECEPTORS, PROCESS FOR PREPARING THEM AND USE THEREOF IN HUMAN MEDICINE AND IN COSMETICS

The invention relates to novel compounds corresponding to formula (I) below: and to the method for preparing them, and to their use in pharmaceutical compositions intended for use in human or veterinary medicine, or alternatively in cosmetic compositions.

Bi-aromatic compounds linked via a heteroethylene radical, and pharmaceutical and cosmetic compositions using them

Bi-aromatic compounds linked via a heteroethynylene radical are provided along with pharmaceutical and cosmetic compositions containing these compounds and methods for their use.

Bi-aromatic compounds linked via a heteroethylene radical, and pharmaceutical and cosmetic compositions using them

Bi-aromatic compounds linked via a heteroethynylene radical are provided along with pharmaceutical and cosmetic compositions containing these compounds and methods for their use.

Bi-aromatic compounds bound by a heteroethynylene radical and pharmaceutical and cosmetic compositions containing same

Bi-aromatic compounds linked via a heteroethynylene radical are provided along with pharmaceutical and cosmetic compositions containing these compounds and methods for their use.