ChemicalBook CAS DataBase List 6-cyclopropyl-8,9-difluoro-7-methoxy-4-oxo-4,6-dihydro-2H-1l3-[1,3]dioxino[5,6-c]quinoline-2,2-diyl diacetate

6-cyclopropyl-8,9-difluoro-7-methoxy-4-oxo-4,6-dihydro-2H-1l3-[1,3]dioxino[5,6-c]quinoline-2,2-diyl diacetate synthesis

7synthesis methods

Product Name:6-cyclopropyl-8,9-difluoro-7-methoxy-4-oxo-4,6-dihydro-2H-1l3-[1,3]dioxino[5,6-c]quinoline-2,2-diyl diacetate
CAS Number:139693-52-0
Molecular formula:C18H16BF2NO8
Molecular Weight:423.13

11113-50-1 Synthesis

11113-50-1
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1-Cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid ethyl ester

112811-71-9
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6-cyclopropyl-8,9-difluoro-7-methoxy-4-oxo-4,6-dihydro-2H-1l3-[1,3]dioxino[5,6-c]quinoline-2,2-diyl diacetate

139693-52-0
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Yield: 99%

Reaction Conditions:

Stage #1:boric acid with acetic anhydride at 90; for 1 h;
Stage #2:ethyl 8-methoxy-1-cyclopropyl-6,7-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylate at 110; for 2 h;Temperature;

Steps:

1.1; 2 Example 2
The rest of the preparation method of moxifloxacin hydrochloride in this example is the same as that in Example 1, except that:Step Preparation of 1-cyclopropyl-6,7-difluoro-8-methoxy-1,4-dihydro-4-oxoquinoline-3-carboxylic acid-O3,O4-diacetic acid boron ester At this time, 558g of acetic anhydride and 70g of boric acid were added to a 3L reaction flask, stirred to dissolve, heated to 90°C for reaction, and stirred at 90°C for 1 hour.After the reaction of acetic anhydride and boric acid is completed, add 300g of 1-cyclopropyl-6,7-difluoro-8-methoxy-1,4-dihydro-4-oxoquinoline-3 into the reaction flask while stirring -Ethyl quinoline carboxylate, heated to 110 for 2h.After the reaction, the temperature of the reaction solution was quickly reduced to 1020. After the crystals were precipitated, 1020 cold water was added for beating for 1 hour. Cyclopropyl-6,7-difluoro-8-methoxy-1,4-dihydro-4-oxoquinoline-3-carboxylic acid-O3,O4-boron diacetate crystals 388g, molar yield The rate is 99%, and the purity is 99.79%.

References:

Changzhou Circumference Pharmaceutical Co., Ltd.;Inner Mongolia Puyin Pharmaceutical Co., Ltd.;Jiang Yanjun;Wang Haidong;Qian Jun;Liu Xin;Lei Xiangxiao;He Yongfei CN111233858, 2020, A Location in patent:Paragraph 0027-0030; 0037-0039