Carboxylic acid compounds and drugs containing the compounds as the active ingredient
A carboxylic acid compound and compound technology, applied in medical preparations containing active ingredients, organic active ingredients, drug combinations, etc., can solve problems such as weak combination and small side effects
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[0186] [Preparation method of the compound of the present invention]
[0187] Compounds of the present invention represented by formula (I) can be prepared by, for example, the following methods:
[0188] [I] In the compound shown in formula (I), R 1 for C 1-4 Alkyl, C 2-4 The compound of alkenyl or benzyl is the compound shown in the following formula (IA)
[0189]
[0190] (where, R 1A for C 1-4 Alkyl, C 2-4 Alkenyl or benzyl, the meaning of other symbols is the same as above) can be prepared by the following method:
[0191] (a) In formula (IA), E represents -C(=O)- or -S(O) 2 The compound of - is formula (IA-1) compound
[0192]
[0193] (where, E A for -C(=O)- or -S(O) 2 -, the meaning of other symbols is the same as above) can be prepared by the following method: formula (II-1) compound
[0194]
[0195] (where, R 2-1 with R 2 have the same meaning, but R 2-1 The hydroxyl or amino group represented is protected when necessary; R 4-1 is a hydrogen at...
Embodiment approach
[0334] The following Reference Examples and Examples are used to illustrate the present invention but not to limit the present invention.
[0335] In chromatographic separation or TLC, the solvents in parentheses represent eluents or developing solvents, and the ratios of solvents used are volume ratios. In NMR, solvents in parentheses are solvents for measurement.
[0336] Reference Example 1: N-formyl-2-fluoroaniline
[0337] To acetic anhydride (15.5 mL) was added dropwise formic acid (6.1 mL) at 0°C under an argon atmosphere, followed by stirring at 50°C for 2 hours. After cooling the reaction mixture to room temperature, it was diluted with tetrahydrofuran (THF; 10 mL). To the above diluted solution was added a solution of 2-fluoroaniline (5.56 g) in THF (20 mL) at room temperature, and the mixture was stirred at room temperature for 1 hr. Concentration of the reaction mixture afforded the title compound having the following physicochemical data. The resulting title c...
Embodiment 1
[0375] Example 1: 3-(4-((2S)-4-methyl-3,4-dihydro-2H-1,4-benzoxazin-2-ylmethoxy)benzoylamino)benzene Methyl acetate
[0376]
[0377] To a solution of the compound prepared in Reference Example 9 (165 mg) in dichloromethane (2 mL) was added pyridine (161 µl) under argon protection. To this mixture was added dropwise a solution of the compound prepared in Reference Example 8 (350 mg) in dichloromethane (2.5 mL) under ice-cooling, and stirred at 0°C for 15 minutes. Methanol and water were added to the mixture. It was extracted with ethyl acetate, and the organic layer was washed with saturated aqueous ammonium chloride and saturated aqueous sodium chloride, dried over anhydrous sodium sulfate, and concentrated to give the title compound (447 mg) having the following physical data.
[0378] TLC: Rf0.23 (hexane:ethyl acetate=2:1).
[0379] Embodiment 1(1)~1(15)
[0380] In the same manner as in Example 1, using the corresponding amine instead of the compound prepared in Ref...
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