Difluoromethyl reaction method and application thereof

A technology of difluoromethylation and difluoromethylation, which is applied in pharmaceutical formulations, medical preparations containing active ingredients, and drug combinations, etc., can solve problems such as limited research on methods and paths, and shortage of related methods.

Active Publication Date: 2022-07-01
SHENZHEN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0011] Although there have been some preliminary research progress and results in this field, the direct C(sp 3 )-H bond difluoromethyl functionalization research methods and pathways are limited, and related methods are in short supply

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  • Difluoromethyl reaction method and application thereof
  • Difluoromethyl reaction method and application thereof
  • Difluoromethyl reaction method and application thereof

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Embodiment Construction

[0046] The technical solutions in the embodiments of the present invention will be clearly and completely described below with reference to the accompanying drawings in the embodiments of the present invention. Obviously, the described embodiments are part of the embodiments of the present invention, but not all of the embodiments. Based on the embodiments of the present invention, all other embodiments obtained by those of ordinary skill in the art without creative efforts shall fall within the protection scope of the present invention.

[0047] It is to be understood that, when used in this specification and the appended claims, the terms "comprising" and "comprising" indicate the presence of described features, integers, steps, operations, elements, but do not exclude one or more other features , the presence or addition of a whole, a step, an operation, an element, and / or a collection thereof.

[0048] It should also be understood that the terminology used in this specific...

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Abstract

The invention discloses a difluoromethyl reaction method and application thereof, and relates to the technical field of medicine preparation. N heterocyclic rings, other amine compounds and a difluoromethyl reagent are adopted to react under the condition of photooxidation reduction catalysis, and construction of C (sp3)-CF2H is completed; the reaction under the photooxidation reduction catalysis condition is that a free radical cross-coupling reaction is carried out in a solvent containing alkali and a photocatalyst under the illumination condition with the wavelength of 350-550 nm, and the reaction time is 10 minutes to 72 hours. According to the method, the cross-coupling reaction of the C (sp3) free radical and the difluoromethyl free radical (. CF2H) is realized, so that the direct difluoromethyl functionalization reaction of C (sp3)-H is completed to construct the C (sp3)-CF2H building block, the method can be used for carrying out difluoromethyl functionalization on 3-site C of 1, 4-dihydroquinoxalinone in a wide range, and the method has the advantages of greenness, environmental protection, economy, convenience, high efficiency and good functional group compatibility.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparation, in particular to a difluoromethyl reaction method and application. Background technique [0002] Difluoroalkyl groups are an important structural moiety widely used in medicine, pesticides and advanced materials. In particular, it has important applications and significance in the design and discovery of drugs, and is widely used in drug development. Difluoromethyl (CF 2 H) is hydroxymethyl (CH) 2 OH), sulfhydryl (SH) and other groups of bioisosteres; in addition, as an important factor affecting the pharmacological activity of the drug and the affinity with the target, the hydrogen bond between the drug molecule and the target protein plays an important role; The hydrogen bond donor difluoromethyl (CF 2 H) has better lipophilicity than hydroxyl (OH) and amino (NH), etc., and can improve the lipid solubility, membrane permeability, bioavailability and other pharmacokinetic ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D241/44A61P35/00A61K31/498
CPCC07D241/44A61P35/00Y02P20/584
Inventor 刘国凯熊威秦文兵
Owner SHENZHEN UNIV
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