226410-00-0Relevant academic research and scientific papers
Synthesis of 2-acyl-3-chloropyrroles: Application to the synthesis of the trail pheromone of the ant Atta texana
Tehrani, Kourosch Abbaspour,Borremans, Didier,De Kimpe, Norbert
, p. 4133 - 4152 (1999)
Alkyl 3-chloropyrrole-2-carboxylates and 2-alkanoyl-3-chloropyrroles are conveniently prepared from 2-alkyl-1-pyrrolines by tetra- and pentahalogenation with N-chlorosuccinimide, subsequent base-induced aromatisation with sodium alkoxides in the corresponding alcohol and final acid hydrolysis of the resulting orthoester or acetal functions into the 3- chloropyrrole. The developed strategy is applied to the synthesis of the trail pheromone of the ant Atta texana.
Synthesis method of 3-chloropyrrole-2-methyl formate
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Paragraph 0014-0021, (2020/06/17)
The invention discloses a synthetic method of 3-chloropyrrole-2-methyl formate. The synthetic method comprises the following steps: firstly, adding 2-methylpyrroline into a dichloromethane solution; reducing the temperature of the reaction liquid to 0-10 DEG C; keeping the temperature at 0-10 DEG C and introducing chlorine into a reaction solution; introducing chlorine gas and performing standingfor 12 to 24 hours at normal temperature; or dissolving 2-methylpyrroline in tetrahydrofuran, performing heating to 55-65 DEG C, controlling the temperature to 55-65 DEG C, adding 1070g of N-chlorosuccinimide in batches, keeping the temperature for 1 hour, performing cooling to room temperature, adding water, performing extracting with petroleum ether for three to five times, and performing concentrating. According to the synthetic method of the 3-chloropyrrole-2-methyl formate, the preparation method is stable and efficient, the preparation rate is stable after an amplification experiment, and expanded production is facilitated.
INHIBITORS OF METALLO-BETA-LACTAMASES
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Paragraph 00261; 00262; 00263, (2018/12/13)
The present invention relates to compounds of Formula (I) that function as inhibitors of bacterial metallo-beta-lactamases. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of a bacterial infection. (Formula (I))
HETEROARYL DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSTION FOR PREVENTING OR TREATING DISEASES ASSOCIATED WITH PI3 KINASES, CONTAINING SAME AS ACTIVE INGREDIENT
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, (2018/04/26)
The present invention relates to a heteroaryl derivative or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a pharmaceutical composition for preventing or treating diseases associated with PI3 kinases, containing the same as an active ingredient. The heteroaryl derivative according to the present invention has an excellent effect of selectively inhibiting PI3 kinases, thereby being useful in preventing or treating PI3 kinase diseases such as: cancers, autoimmune diseases, and respiratory diseases.
Pyrimido oxazine derivatives or pharmaceutically acceptable salts thereof, preparation method thereof and pharmaceutical composition for use in preventing or treating PI3 kinase related diseases
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, (2017/08/02)
The present invention relates to pyrimido oxazine derivatives or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition comprising the same as an effective component for preventing or treating PI3 kinase-related diseases. The pyrimido oxazine derivatives according to the present invention have excellent selective inhibitory effects on PI3 kinase, and thus may be beneficially used in preventing or treating PI3 kinase-related diseases such as the following: cancers including blood cancer, ovarian cancer, cervical cancer, breast cancer, large intestine cancer, liver cancer, stomach cancer, pancreatic cancer, colon cancer, periotoneal cancer, skin cancer, bladder cancer, prostate cancer, lung cancer, osteosarcoma, fibrous tumor, and brain tumor; autoimmune diseases including rheumatoid arthritis, systemic lupus erythematosus, multiple sclerosis, type 1 diabetes, hyperthyroidism, myasthenia gravis, Crohnandprime;s disease, ankylosing spondylitis, psoriasis, pernicious anemia, and Sjogrenandprime;s syndrome; and respiratory diseases including chronic obstructive pulmonary disease (COPD), rhinitis, asthma, chronic bronchitis, chronic pulmonary inflammatory diseases, silicosis, pulmonary sarcoidosis, pleuritis, alveolitis, vasculitis, emphysema, pneumonia, and bronchiectasis.COPYRIGHT KIPO 2017
COMPOSITIONS USEFUL FOR TREATING DISORDERS RELATED TO KIT
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Paragraph 0192; 0193, (2015/04/28)
Compounds and compositions useful for treating disorders related to mutant KIT are described herein.
NOVEL HETEROARYL AND HETEROCYCLE COMPOUNDS, COMPOSITIONS AND METHODS
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, (2014/02/16)
Provided are novel heteroaryl and heterocycle compounds of formula (I-1), (I-2) or (I-3) and pharmaceutical compositions comprising them, uses and methods thereof for inhibiting the activity of PI3K and for treating inflammatory and autoimmune disorders diseases and cancer.
NOVEL HETEROARYL AND HETEROCYCLE COMPOUNDS, COMPOSITIONS AND METHODS
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, (2014/02/16)
The invention relates to novel heteroaryl and heterocycle compounds and pharmaceutical compositions comprising them, uses and methods thereof for inhibiting the activity of PI3k and for treating inflammatory and autoimmune disorders diseases and cancer.
NOVEL HETEROARYL AND HETEROCYCLE COMPOUNDS, COMPOSITION AND METHODS THEREOF
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, (2014/02/16)
Disclosed are novel heteroaryl and heterocycle compounds of formula I-1, I-2 or I-3 and pharmaceutical compositions comprising them, uses and methods thereof for inhibiting the activity of PI3K and for treating inflammatory and autoimmune diseases and cancer.
PYRROLOTRIAZINES AS POTASSIUM ION CHANNEL INHIBITORS
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Page/Page column, (2014/09/29)
A compound of formula (I) wherein A, R1, R3, and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment of arrhythmia, maintaining normal sinus rhythm, IKur-associated disorders, and other disorders mediated by ion channel function.
