122 results about "Indolizine" patented technology

Compounds of formula (I), defined herein, inhibit phosphoinositide 3-kinases (PI3K) and are useful for the treatment of disorders associated with PI3K enzymes.

The invention provides a simple preparation method of a 3-aryl indolizine derivative. The method comprises the following step of: reacting N-benzylpyridine onium salt directly prepared from a pyridine derivative and benzyl halide with electron-deficient alkyne under the existence of alkali to prepare the 3-aryl indolizine derivative. All raw materials used in the simple preparation method can be directly purchased, and are relatively low in price and easy to obtain; any catalyst, ligand and oxidant do not need to be used in the process flow, the process flow is simple, and the cost is obviously reduced; the problem that transition metal in target products exceeds standards is avoided; the whole process is insensitive to air or moisture, and the normal operation can be carried out under loose reaction conditions without polluting the environment; and the simple preparation method can be used for providing the 3-aryl indolizine derivative with abundant sources and low price for the preparation of related products in the fields of biology, pesticides and medicine.

The invention discloses a method for preparing a 3-aryl purrocoline derivative. The 3-aryl purrocoline derivative is prepared by arylboronic acid in the presence of a palladium catalyst based on oxygen as a final oxidant. The process comprises the following steps of: placing purrocoline substituted by hydrogen in site 3, arylboronic acid, the palladium catalyst, nitrogen-containing ligands or nitrogen-free ligands and alkaline components in a reactor utensil according to a molar ratio of 1:(1.0-3.0):(0.0125-0.10):(0.0125-0.30) or 0.0:(1.0-5.0); adding 2.0-20ml of solvent; heating and stirring under oxygen atmosphere to react; pouring a mixture after reaction to water; and filtering, washing and drying, and recrystalizing or performing column chromatography isolation to obtain the 3-aryl purrocoline derivative. The method provided by the invention is short in process flow, simple and accessible, and the nitrogen--containing ligands or nitrogen-free ligands which are not expensive can be selected. The final oxidant is oxygen in air which is green and environment-friendly, so that the reaction condition is loose, the preparation cost is lowered, and the 3-aryl purrocoline derivative in rich source can be provided for manufacturing related products in the field of biology, pesticides and medicines.

The present invention is directed to compounds of formula (I):described as novel indolizine derivatives and to a method for their preparation along with pharmaceutical compositions thereof whose substituents are as described in the specification.

The invention discloses an indolizine carboxylic acid pH fluorescent probe, the probe is 2-acetyl indolizine-7-carboxylic acid, and its chemical structural formula is shown in formula (1). The fluorescent probe of the present invention has unique fluorescence selectivity and higher sensitivity to pH in an aqueous solution of dimethyl sulfoxide. Compared with existing probes, it has a narrow pH corresponding range and is not subject to background interference. It is suitable for It has significant advantages such as pH detection in strongly acidic environments, and has great application prospects.

The invention relates to a pH-responsive fluorescent molecular probe with a chemical name, namely, 5-(2-phenyl-pyrrolo[2,1,5-cd]indolizine-5-yl)-1,3,4-oxadiazole-2-thiophenol, as well as a preparation method and application thereof. According to the preparation method, a mercapto group is adopted as an identifying group and an indolizine group is adopted as a signal group for the first time to successfully prepare the compound. By virtue of the fluorescent probe molecules, a sensitive identification of H<+1> under different pH values is realized, the types of the pH-responsive fluorescent molecular probe are enriched, and a novel use of the mercapto functional group is opened up. The pH-responsive fluorescent molecular probe has very broad industrial application prospects and provides valuable reference to make a scientific research.