154411-16-2

Upstream product

• 495-69-2 Hippuric Acid 
• 2739-97-1 pyridine-2-acetonitrile 
• 1188-33-6 N,N-dimethylformamide diethyl diacetal 
• 125008-68-6 methyl (Z)-2-benzoylamino-3-dimethylaminopropenoate 

Relevant academic research and scientific papers

Intermediate products, methods for their preparation and use thereof

Novel solid supported intermediate products of the general formula coupled to a solid polymeric support through one or both of the R1 groups or through the R4 group which are suitable for synthesis of heterocyclic compounds are disclosed. Methods for preparing such intermediate products are also disclosed and also the use of the intermediate products in simple and fast methods on solid phase for synthesis of heterocycles.

Solid phase synthesis of aminopropenones and aminopropenoates; efficient and versatile synthons for combinatorial synthesis of heterocycles

Simple and fast solid phase methods for the synthesis of heterocycles will be described. Two different three-step methods are presented. The first method includes esterifications of N-protected glycine derivatives to a solid support (Merrifield resin), formation of aminopropenoates and subsequent reaction with dinucleophiles. The second method includes methylamination of a Merrifield resin, formation of aminopropenones via in-situ formation of an active intermediate in a three-component reaction and finally treatment with dinucleophiles to form heterocycles. These procedures lead not only to the formation of heterocycles but also to simultaneous intramolecular cleavage of the products from the resin giving the product in pure form in the solution. In addition, the use of microwave dielectric heating enhanced the velocity of all reaction steps and was found to be a very efficient complement to the solid phase synthesis.

Amino Acids in the Synthesis of Heterocyclic Systems. The Synthesis of 4-Oxo-4H-pyridopyridines and 4-Oxo-4H-pyridopyrimidines

The pyridine and quinoline derivatives 2, 3, and 6 with an activated methylene group at α-position in respect to the ring nitrogen atom were converted with 1, 8, or 9 into fused pyridopyridine derivatives 4, 5, 7, and 10.In an analogous manner were the aminopyridines 16 and 17 transformed with thiazolone 9 into pyridopyrimidine derivatives 20, 21, 25, and 26.