CAS: 1620097-06-4; (R)-1-Benzyl-5-Methyl-1,4-Diazepane

相似化合物

1001401-60-0 1638744-15-6 150651-61-9

N-苄基甘氨酸置于盐酸,Lithium Aluminium Tetrahydride,氯化亚砜,Sodium Methylate,1-羟基苯并三唑,盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺,三乙胺体系中,用 四氢呋喃,甲醇,乙酸乙酯,N,N-二甲基甲酰胺 用作溶剂,化学反应 75.5H,反应生成(5R)-六氢-5-甲基-1-苄基-1H-1,4-二氮杂卓
参考文献:潜在食欲素受体拮抗剂氮杂环庚烷磺酰胺衍生物的合成及生物活性评价
标题:潜在食欲素受体拮抗剂氮杂环庚烷磺酰胺衍生物的合成及生物活性评价
摘要:由于食欲素信号系统对调节睡眠/觉醒周期至关重要,因此食欲素1和食欲素2受体的抑制剂在失眠症的治疗中具有重要意义.在此,设计并合成了一系列新型氮杂环庚烷磺酰胺衍生物,并通过 Flipr Tetra 钙测定法评估了所有化合物作为潜在的食欲素受体抑制剂.大多数测试的氮杂环庚烷磺酰胺衍生物显示出ox1R和ox2R抑制活性.在苯并恶唑基团的 C5 或 C6 位置官能化的氯取代衍生物对 Ox1R 和 Ox2R 表现出比在 C5 或 C6 官能化的未取代衍生物更好的抑制活性.此外,苯基修饰对抑制活性有积极影响,并且在苯环的邻位或间位提高了衍生物的ox2R抑制活性.这表明氮杂环庚烷磺酰胺衍生物是开发 Ox1R 和 Ox2R 拮抗剂的有前途的支架.
Doi:10.1039/d0Ra05068G

专利信息

专利号:US-2016168138-A1
优先权日:2013-07-15
标题:Process for the preparation of suvorexant and intermediates useful in the synthesis of suvorexant
发明人：IQBAL JAVED; DAHANUKAR VILAS HARESHWAR; ORUGANTI SRINIVAS; KANDAGATLA BHASKAR
权利人:REDDY S LAB LIMTED DR
摘要:A novel processes for the preparation of suvorexant (formula I), its related compounds and its intermediates that are simple, economical and commercially viable. (I)

专利号:EP-3021851-A2
优先权日:2013-07-15
标 题 :Process for the preparation of suvorexant and intermediates useful in the synthesis of suvorexant

专利号:US-10618891-B2
优先权日:2016-02-01
标 题 :Suvorexant intermediate and preparation method thereof
发明人：LIN JIANPING; GUO XIAOWEN; GAO XIAOFEI; HUANG CHAO; GUO YUANBING; TAO ANPING; HUANG LUNING; GU HONG
权利人:ZHEJIANG HUAHAI PHARM CO LTD; SHANGHAI AOBO PHARMTECH INC LTD
摘要:The present invention relates to a synthesis process of suvorexant, novel compounds represented by formulas II, III, IV or V, or salts thereof for preparing suvorexant, and a method for preparing the intermediates. The preparation method uses a chiral starting material to synthesize chiral compounds represented by formulas II, III, IV or V, the compounds obtained being used for synthesizing the suvorexant. The preparation method has the advantages of simple operation, low cost, mild reaction conditions, simple post-treatment, easy to purify, high yield, high ee value for the product, and easy to industrialize. In the reaction route shown, R represents benzyl, allyl or 1-phenethyl, or optionally substituted benzyl at the 2 position to 6 position, such as 4-methoxybenzyl, 4-nitrobenzyl, 2-methylbenzyl, 4-chlorobenzyl or 3-fluorobenzyl.