アトゲパント 価格

メーカー	製品番號(hào)	製品説明	CAS番號(hào)	包裝	価格	更新時(shí)間	購(gòu)入

アトゲパント 化學(xué)特性,用途語(yǔ),生産方法

効能

抗片頭痛薬, カルシトニン受容體様受容體拮抗薬

使用

Atogepant (MK-8031) is an orally active and selective calcitonin gene–related peptide receptor (CGRP) antagonist. Atogepant can be used for researching migraine.

副作用

The side effect profile of atogepant is similar to other gepants, most frequently including constipation, nausea, upper respiratory and urinary tract infection, and appearing similarly in long-term follow-up studies and clinical trials. Currently, there is no data on the safety of atogepant treatment during pregnancy or lactation. However, it can be assumed, based on animal data, that it is able to pass into breast milk.

合成

The synthesis of atogepant was carried out via amide coupling of two advanced intermediate fragments. The specific route is as follows:
Step 1: The synthesized carboxylic acid fragment started from the biscarboxylic acid 10.1, which was converted to the bisester under acidic conditions and then brominated to give the bromopyridine 10.2 (Fig. 1). 10.3 was obtained by reduction of the two esters and subsequent mesylation. Treatment of the mesylate 10.3 with the pyridone 10.4 under basic conditions gave the racemic spirocyclic compound 10.5. Palladium-catalyzed carbonylation gave the methyl ester, which was purified by chiral supercritical fluid chromatography (SFC) to give the single enantiomer pyridine 10.6. Ester hydrolysis and deprotection of the SEM protecting group gave the desired carboxylic acid fragment 10.7.

Step 2: The amine fragment synthesis was performed by converting the carboxylic acid 10.11 to the corresponding Weinreb amide 10.12 (N-methoxy-N-methylamide) by generating the acid chloride using POCl3 (Fig. 2). The Weinreb amide reacted with the Grignard reagent methylmagnesium chloride to give the methyl ketone 10.13. Enolization of the ketone 10.13 was achieved using LiOt-Bu and ZnBr2. Subsequently, treatment with the racemic mesylate 10.14 gave the amino acid derivative 10.15. Enzymatic reductive amination of the ketone 10.15 and transaminase-induced cyclization gave the pyridone 10.16 with a >60:1 cis-trans ratio at C5:C6 and a 1:1 mixture of cis-trans isomers at C3. Epimerization of 10.16 with t-BuOK gave the pyridone 10.17. Selective N-alkylation with the triflate 10.18 gave the pyridone 10.19 with a 6.5:1 mixture of cis-trans isomers at the C3 position. The primary amine at the C3 position was obtained by acidic deprotection and then treated with amino acid 10.20 to generate salt 10.21. Finally, amine 10.21 was treated as a free base and reacted with carboxylic acid 10.7 via EDC coupling to afford Atogepant (10) in 95% yield.

アトゲパント 上流と下流の製品情報(bào)

原材料

準(zhǔn)備製品

アトゲパント 生産企業(yè)

名前	電話番號(hào)	電子メール	國(guó)籍	製品カタログ	優(yōu)位度
Wuhan Jingkang en Biomedical Technology Co., Ltd	+86-0086-13720134139	orders@jknbiochem.com	China	5221	58
shandong perfect biotechnology co.ltd	+86-53169958659 +86-13153181156	sales@sdperfect.com	China	294	58
ZHENGZHOU JIUYI TIME NEW MATERIALS CO,.LTD	+86-15225627621 +86-13213167925	jiuyitime@fdachem.com	China	16511	58
Shanghai Daken Advanced Materials Co.,Ltd	+86-2158073036	info@dakenam.com	China	14026	58
Jinan Carbotang Biotech Co.,Ltd.	+8615866703830	figo.gao@foxmail.com	China	8497	58
SHANGHAI T&W PHARMACEUTICAL CO., LTD.	+86-021-61551413	contact@trustwe.com	China	5746	58
TargetMol Chemicals Inc.	+1-781-999-5354; +1-00000000000	marketing@targetmol.com	United States	32468	58
HANGZHOU CLAP TECHNOLOGY CO.,LTD	86-571-88216897,88216896 13588875226	sales@hzclap.com	CHINA	6312	58
Zhejiang J&C Biological Technology Co.,Limited	+1-2135480471	sales@sarms4muscle.com	China	10457	58
SyncoZymes (Shanghai) Co., Ltd.,	+86-13681683526（Wechat）	lchen@syncozymes.com	China	286	58

1374248-81-3(アトゲパント)キーワード:

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• 1374248-81-3
• MK-8031
• Spiro[6H-cyclopenta[b]pyridine-6,3'-[3H]pyrrolo[2,3-b]pyridine]-3-carboxamide, 1',2',5,7-tetrahydro-N-[(3S,5S,6R)-6-methyl-2-oxo-1-(2,2,2-trifluoroethyl)-5-(2,3,6-trifluorophenyl)-3-piperidinyl]-2'-oxo-, (3'S)-
• (S)—N-((3S,5S,6R)-6-methyl-2-oxo-1-(2,2,2-trifluoroethyl)-5-(2,3,6-trifluorophenyl)piperidin-3-yl)-2’-oxo-1’,2’,5,7-tetrahydrospiro[cyclopenta[b]pyridine-6,3’-pyrrolo[2,3-b]pyridine]-3-carboxamide
• (S)—N-((3S,5S,6R)-6-methyl-2-oxo-1-(2,2,2-trifluoroethyl)-5-(2,3,6-trifluorophenyl)piperidin-3-yl)-2'-oxo-1',2',5,7-tetrahydrospiro[cyclopenta[b]pyridine-6,3'-pyrrolo[2,3-b]pyridine]-3-carboxamid
• MK8031. Atogepant
• Atogepant API
• (S)-1'-(tert-butyl)-N-((3S,5S,6R)-6-methyl-2-oxo-1-(2,2,2-trifluoroethyl)-5-(2,3,6-trifluorophenyl)piperidin-3-yl)-2'-oxo-1',2',5,7-tetrahydrospiro[cyclopenta[b]pyridine-6,3'-pyrrolo[2,3-b]pyridine]-3-carboxamide
• (3'S)-N-[(3S,5S,6R)-6-methyl-2-oxo-1-(2,2,2-trifluoroethyl)-5-(2,3,6-trifluorophenyl)piperidin-3-yl]-2'-oxo-1',2',5,7-tetrahydrospiro[cyclopenta[b]pyridine-6,3'-pyrrolo[2,3-b]pyridine]-3-carboxamide
• (3'S)-1',2',5,7-tetrahydro-N-[(3S,5S,6R)-6-methyl-2-oxo-1-(2,2,2-trifluoroethyl)-5-(2,3,6-trifluorophenyl)-3-piperidinyl]-2'-oxo-Spiro[6H-
• (S)-N-((3S,5S,6R)-6-Methyl-2-oxo-1-(2,2,2-trifluoroethyl)-5-(2,3,6-trifluorophenyl)piperidin-3-yl)-2'-oxo-1',2',5,7-tetrahydrospiro[cyclopenta[b]pyridine-6,3'-pyrrolo[2,3-b]pyridine]-3-carboxamide
• AGN-241689）
• (S)-N-[(3S,5S,6R)-6-Methyl-2-oxo-1-(2,2,2-trifluoroethyl)-5-(2,3,6-trifluorophenyl)piperidin-3-yl]-2'-oxo-1',2',5,7-tetrahydrospiro[cyclopenta[b]pyridine-6,3'-pyrrolo[2,3-b]pyridine]-2-carboxamide
• Atogepant Monohydrate
• Atogypam
• (3′S)-1′,2′,5,7-Tetrahydro-N-[(3S,5S,6R)-6-methyl-2-oxo-1-(2,2,2-trifluoroethyl)-5-(2,3,6-trifluorophenyl)-3-piperidinyl]-2′-oxospiro[6H-cyclopenta[b]pyridine-6,3′-[3H]pyrrolo[2,3-b]pyridine]-3-carboxamide (ACI)
• アトゲパント