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P310
즉시 의료기관(의사)의 진찰을 받으시오.
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P321
(…) 처치를 하시오.
P330
입을 씻어내시오.
P332+P313
피부 자극이 생기면 의학적인 조치· 조언을 구하시오.
P362
오염된 의복을 벗고 세척 후에 재사용하기
P501
...에 내용물 / 용기를 폐기 하시오.
Methyl 4-Fluoro-2-{1H-pyrrolo[2,3-b]pyridin-5-yloxy}benzoate C화학적 특성, 용도, 생산
용도
Methyl 4-Fluoro-2-{1H-pyrrolo[2,3-b]pyridin-5-yloxy}benzoate is the intermediate for ABT 199 (A112430), which is a potent and selective BCL-2 inhibitor that achieves potent antitumor activity while sparing platelets. It’s practical application is to treat chronic lymphocytic leukaemic cells and estrogen receptor-positive breast cancer.
Synthesis
Methyl 4-Fluoro-2-{1H-pyrrolo[2,3-b]pyridin-5-yloxy}benzoate is prepared by the reaction of 5-Hydroxy-7-azaindole and Methyl 2,4-difluorobenzoate
. The specific synthesis steps are as follows: To a three-necked flask was added 100 g of 5-hydroxy-7-azaindole (746 mmol), 141 g of methyl 2,4-difluorobenzoate(821 mmol), 237 g of potassium phosphate (1.12 mol) and 500 mL of diethylene glycol dimethyl Ether, 110 ° C for 24 h (HPLC to monitor 5-hydroxy-7-azaindole).The reaction solution was concentrated to dryness, and 2L of ethyl acetate and 2 L of water were added. The organic phase was separated,dried over anhydrous sodium sulfate, and concentrated to dry crude.The crude product was heated to reflux with 1260 mL of ethyl acetate. The mixture was slowly added dropwise to a solution of 1260 mL ofpetroleum ether. After 1 h of dropping, the mixture was stirred for 1 h, slowly cooled to 25 ° C, filtered and dried to give163g of pale white solidRate of 76.5percent.HPLC purity 98percent.
Methyl 4-Fluoro-2-{1H-pyrrolo[2,3-b]pyridin-5-yloxy}benzoate 준비 용품 및 원자재
![Methyl 4-Fluoro-2-{1H-pyrrolo[2,3-b]pyridin-5-yloxy}benzoate synthesis](/NewsImg/2024-04-03/6384773502334631747821437.png "Methyl 4-Fluoro-2-{1H-pyrrolo[2,3-b]pyridin-5-yloxy}benzoate synthesis")