CAS: 608141-42-0; (S)-1-(3-Ethoxy-4-Methoxyphenyl)-2-(Methylsulfonyl)Ethanamine

上下游产品

阿普斯特中间体 2-(3-Ethoxy-4-Methoxyphenyl)-1-(Methylsulphonyl)-Eth-2-Ylamine 253168-94-4
阿普斯特中间体 (R)-1-(3-Ethoxy-4-Methoxyphenyl)-2-(Methylsulfonyl)Ethanamine 608142-27-4
(S)-4-(1-Azido-2-(Methylsulfonyl)Ethyl)-2-Ethoxy-1-Methoxybenzene 1450657-43-8
1-(3-Ethoxy-4-Methoxyphenyl)-2-(Methylsulfonyl)-N-(Trimethylsilyl)Ethylamine 1255909-21-7
(S)-1-(3-Ethoxy-4-Methoxyphenyl)-2-(Methylsulfonyl)-N-((S)-1-Phenylethyl)Ethylamine
(S)-1-(3-Ethoxy-4-Methoxyphenyl)-2-(Methylsulfonyl)Ethanamine 1450657-40-5
(R)-1-(3-乙氧基-4-甲氧基苯基)-2-(甲磺酰基)-1-乙醇 (R)-1-(3-Ethoxy-4-Methoxyphenyl)-2-(Methylsulfonyl)Ethanol 1450657-24-5
1-(3-乙氧基-4-甲氧基苯基)-2-(甲磺酰基)乙酮 1-(3-Ethoxy-4-Methoxyphenyl)-2-(Methylsulfonyl)Ethanone 1450657-28-9
1-(3-乙氧基-4-甲氧基苯基)乙酮 3-Ethoxy-4-Methoxy-Acetophenone 31526-71-3

3-乙氧基-4-甲氧基苯甲酸甲酯置于palladium 10% On Activated Carbon,氢气,四氯化钛,Sodium Hydride,对甲苯磺酸体系中,用 甲醇,正己烷,环己烷 作为反应溶剂,35.0 °C,300.01 Kpa 条件下,反应 7.0H,反应生成 (Alphas)-3-乙氧基-4-甲氧基-Alpha-[(甲基磺酰基)甲基]-苯甲胺
参考文献:一种合成阿普斯特中间体的制备方法
标题:一种合成阿普斯特中间体的制备方法
摘要:本发明涉及一种合成阿普斯特中间体的制备方法.该方法是利用3-乙氧基-4-甲氧基-苯甲酸酯和二甲基砜在碱性条件下缩合反应反应生成2-(3-乙氧基-4-甲氧基苯)基-1-甲磺酰基乙酮(ⅱ);该化合物ⅱ与手性胺在酸性催化剂存在下反应得到1-N-取代氨基-1-(3-乙氧基-4-甲氧基)苯基-2-甲磺酰基乙烯(ⅲ),所得化合物ⅲ不经过分离直接在加氢催化剂存在下氢化,得到产品(S)-1-(3-乙氧基-4-甲氧基)苯基-2-甲基磺酰基乙胺(I),即为阿普斯特中间体,也可进一步制成n-乙酰氨基l-亮氨酸盐.本发明还提供阿普斯特的制备方法.本发明工艺流程简洁,安全环保,成本低,利于清洁的工业化生产.

专利信息

专利号:WO-2016192694-A1
优先权日:2015-06-05
标 题 :A process for preparing the key intermediate of apremilast, using enzymatic resolution of the racemic amines
发明人：DOUBSKY JAN; KLVANA ROBERT; RICHTER JINDRICH; Lehnert Petr
权利人:ZENTIVA KS
摘要:The invention relates to a preparation method of (S)-l-(3-ethoxy-4-methoxyphenyl)- 2-(methylsulfonyl)-ethyl-amine (S)-l, or its N-acyl derivatives of general formula (S)-2. The amine (S)-l is the key intermediate in the synthesis of (S)-{2-[l-(3-ethoxy-4- methoxyphenyi)-2-methyisulfonylethyl]-4-acetylaminoisoindolin-l ?3-dione, known as Apremilast. In this synthesis, the amine (S)-l, or its respective salts, are subjected to condensation with 3-acetamidophthalic anhydride 4, providing the desired product 3 (Scheme 1).

专利号:US-8242310-B2
优先权日:2008-09-10
标题:Processes for the preparation of aminosulfone compounds
发明人：SAINDANE MANOHAR T; GE CHUANSHENG
权利人:SAINDANE MANOHAR T; GE CHUANSHENG; CELGENE CORP
摘要:Processes for synthesizing aminosulfone compounds are provided. Aminosulfone compounds obtained using methods provided herein are useful in production or synthesis of isoindoline based PDE 4 modulators.

专利号:US-9688623-B2
优先权日:2012-02-21
标题:Processes for the preparation of (S)-1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethylamine
发明人：VENKATESWARALU JASTI; RAJENDIRAN CHINNAPILLAI; REDDY NALLAMADDI RAVIKUMAR; CONNOLLY TERRENCE JOSEPH; RUCHELMAN ALEXANDER L; ECKERT JEFFREY; FRANK ANTHONY JOSEPH
权利人:CELGENE CORP
摘要:Provided herein are new processes for the preparation of aminosulfone intermediates for the synthesis of 2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, which is useful for preventing or treating diseases or conditions related to an abnormally high level or activity of TNF-α. Further provided herein are processes for the commercial production of (S)-1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethylamine.

专利号:US-9126906-B2
优先权日:2012-02-21
标 题:Asymmetric synthetic processes for the preparation of aminosulfone compounds
发明人：CONNOLLY TERRENCE J; RUCHELMAN ALEXANDER L; LEONG WILLIAM W
权利人:CELGENE CORP
摘要:Processes for synthesizing aminosulfone compounds are provided. The processes provided herein utilize asymmetric reduction reactions, e.g., asymmetric hydrogenation, of protected or unprotected enamine or ketone substrates. Aminosulfone compounds obtained using methods provided herein are useful in production or synthesis of sulfone group containing isoindoline based compounds.

专利号:WO-2016202806-A1
优先权日:2015-06-15
标题:A novel synthetic pathway towards apremilast
发明人：STAVBER GAJ
权利人:LEK PHARMACEUTICALS
摘要:The present invention relates to a process for providing a chiral β-hydroxysulfone compound, an intermediate useful in the synthesis of the isoindoline-based compound apremilast.

专利号:EP-3280701-B1
优先权日:2015-04-09
标 题 :A method of chiral resolution of the key intermediate of the synthesis of apremilast and its use for the preparation of pure apremilast
发明人：FAIGL FERENC; DOUBSKY JAN; KLVANA ROBERT; RICHTER JINDRICH; FOGASSY ELEMER; MATRAVOLGYI BELA; MIZSAK AGNES
权利人:ZENTIVA KS