올무티닙

한글명:올무티닙

카스 번호1353550-13-6

상품명:Olmutinib

CBNumberCB83049541

분자식C26H26N6O2S

포뮬러 무게486.59

MOL 파일1353550-13-6.mol

동의어(한글)

올무티닙

화학적 성질

밀도	1.336±0.06 g/cm3(Predicted)
저장 조건	Store at -20°C
용해도	insoluble in H2O; ≥9.11 mg/mL in EtOH with ultrasonic; ≥96.6 mg/mL in DMSO
물리적 상태	결정질 고체
산도 계수 (pKa)	12.87±0.70(Predicted)
색상	Light yellow to yellow

그림문자(GHS)

그림문자(GHS)
신호 어

Warning
유해·위험 문구

H315：피부에 자극을 일으킴

H319：눈에 심한 자극을 일으킴

H335：호흡 자극성을 일으킬 수 있음
예방조치문구

P261：분진·흄·가스·미스트·증기·...·스프레이의 흡입을 피하시오.

P264：취급 후에는 손을 철저히 씻으시오.

P264：취급 후에는 손을 철저히 씻으시오.

P271：옥외 또는 환기가 잘 되는 곳에서만 취급하시오.

P280：보호장갑/보호의/보안경/안면보호구를 착용하시오.

P302+P352：피부에 묻으면 다량의 물로 씻으시오.

P304+P340：흡입하면 신선한 공기가 있는 곳으로 옮기고 호흡하기 쉬운 자세로 안정을 취하시오.

P305+P351+P338：눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.

P312：불편함을 느끼면 의료기관(의사)의 진찰을 받으시오.

P321：(…) 처치를 하시오.

P332+P313：피부 자극이 생기면 의학적인 조치· 조언을 구하시오.

P337+P313：눈에 대한 자극이 지속되면 의학적인 조치· 조언를 구하시오.

P403+P233：용기는 환기가 잘 되는 곳에 단단히 밀폐하여 저장하시오.

P405：밀봉하여 저장하시오.

P501：...에 내용물 / 용기를 폐기 하시오.

올무티닙 화학적 특성, 용도, 생산

개요
Olmutinib, codeveloped by Boehringer Ingelheim and Hanmi Pharmaceutical Co., was approved by the Korean Ministry of Food and Drug Safety (MFDS) for treatment of locally advanced or metastatic EGFR T790 M mutation-positive non-small cell lung cancer (NSCLC). Olmutinib serves as a third-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR TKI), which is being used as an oral therapy for patients who have previously been treated with an alternate EGFR TKI. Firstand second-generation EGFR TKIs, which bind reversibly and irreversibly to the TK domain, respectively, are both generally effective at onset of treatment but result in development of resistance within the first year of treatment. Thirdgeneration EGFR TKIs such as olmutinib have demonstrated the ability to covalently bind to the kinase domain of EGFR while sparing wild-type EGFR, leading to irreversible inhibition of both EGFR mutations and the T790 M mutation, which is linked to EGFR TKI resistance.
용도
Olmutinib is an epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) against non-small cell lung cancer (NSCLC).
Synthesis
Synthetically, olmutinib can be accessed in two steps beginning with 2,4-dichloro-thieno[3,2-d]pyrimidine (147), which is commercially available and can be prepared in two steps from urea and 3-aminothiophene 2- carboxylate. Nucleophilic addition of N-(3-hydroxyphenyl)-2- propenamide (148) to 147 proceeded with complete regioselectivity via treatment with K2CO3 in warm DMSO, smoothly providing the desired diaryl ether 149 in 87% yield after crystallization from isopropanol and water. From 149, substitution with commercially available piperazinyl aniline 150 under acidic heating conditions (DMA, IPA, TFA, 90 ??C) provided olmutinib in 82% yield. After recrystallization, olmutinib (XVI) was obtained in 60% overall yield and 99.1% purity.

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