- Preparation method of carboxylic ester compound
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The invention relates to a preparation method of a carboxylic ester compound, which comprises the following steps: reacting carboxylic acid with methanol in air under the catalysis of nitrite to obtain an ester compound, the preparation method disclosed by the invention has the advantages of rich raw material sources, cheap and easily available catalyst, mild reaction conditions, simplicity and convenience in operation and the like, a series of fatty carboxylic acids can be modified with high yield, and particularly, the traditional esterification method is generally not suitable for esterification of drug molecules. By utilizing the method, a series of known drug molecules can be modified, so that a shortcut is provided for discovering new drug molecules.
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Paragraph 0036-0037
(2021/03/30)
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- Green Esterification of Carboxylic Acids Promoted by tert-Butyl Nitrite
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In this work, the green esterification of carboxylic acids promoted by tert-butyl nitrite has been well developed. This transformation is compatible with a broad range of substrates and exhibits excellent functional group tolerance. Various drugs and substituted amino acids are applicable to this reaction under near neutral conditions, with good to excellent yields.
- Cheng, Xionglve,Jiang, Gangzhong,Li, Xingxing,Tao, Suyan,Wan, Xiaobing,Zhao, Yanwei,Zheng, Yonggao
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supporting information
p. 2713 - 2718
(2021/06/25)
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- A PROCESS FOR THE SYNTHESIS OF OLOPATADINE
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The present invention provides a process for the synthesis of olopatadine. Further, the invention discloses a process that results in improved yield of the desired Z isomer.
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Paragraph 0019
(2014/10/03)
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- A simple synthesis of the novel antihistaminic drug olopatadine hydrochloride
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A new alternative route for the synthesis of olopatadine is described. The present strategy involves a Lewis acid mediated ring opening of a cyclic ether to introduce 3-(dimethylamino)propylidene group as the side chain. Georg Thieme Verlag Stuttgart . New York.
- Chavan, Subhash P.,Lasonkar, Pradeep B.
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p. 3399 - 3403
(2014/01/06)
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- TRICYCLIC COMPOUNDS
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Novel tricyclic compound represented by formula STR1 possess a TXA. sub.2 biosynthesis inhibiting activity and/or a TXA 2 receptor antagonizing activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.
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- Tricyclic compounds
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Novel tricyclic compounds having a TXA2 -antagonizing activity represented by formula (I): STR1 which strongly antagonize an action of thromboxane A2 and are expected to have preventive and therapeutic effects on ischemica diseases, cerebro-vascular diseases, etc.
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- 6,11-dihydrodibenz[b,e]oxepin-acetic acids and derivatives
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6,11-Dihydrodibenz[b,e]oxepin-acetic acids and derivatives having the general formula STR1 are prepared by multi-step sequences. X is C=O, CHCl, CHBr, CH2 or CHOR4 ; Y is alkyl or alkoxy of 1 to 4 carbon atoms, halogen or trifluoromethyl; n is 0, 1, 2 or 3; Z is COOR5, CH2 OR5, CONR25 or CONHOR5 ; and R1 -R5 are hydrogen or alkyl of 1 to 4 carbon atoms. These compounds and the physiologically tolerable salts thereof are useful as antiinflammatory and analgesic agents.
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