1103738-19-7

基本信息
LX4211中間體
6AS)-6-羥基-2
2-二甲基四氫呋喃并[2
99.5%索格列凈中間體
3]二氧雜環(huán)戊烯-5-基)(嗎啉代)甲酮
(5S)-4,5-O-(1-甲基亞乙基)-1-C-4-嗎啉基-D-戊二醛-5,2-呋喃木糖
((3AS,5R,6S,6AS)-6-羥基-2,2-二甲基四氫呋喃并[2,3-D] [1,3]二氧雜
((3AS,5R,6S,6AS)-6- 羥基-2,2- 二甲基四氫呋喃基[2,3-D][1,3]二氧雜-5-基)嗎啉
((3AS,5R,6S,6AS)-6-羥基-2,2-二甲基四氫呋喃并[2,3-D][1,3]二噁戊環(huán)-5-基)(嗎啉代)甲酮
EOS-61383
LX-4211 int
6aS)-6-hydroxy-2
LX-4211 inermediate
LX-4211 intermediate
2-dimethyltetrahydrofuro[2
3]dioxol-5-yl)(morpholino)methanone
(5S)-4,5-O-(1-Methylethylidene)-1-C-4-morpholinyl-D-xylo-pentodialdo-5,2-furanose
D-xylo-Pentodialdo-5,2-furanose, 4,5-O-(1-Methylethylidene)-1-C-4-Morpholinyl-,(5S)-
物理化學(xué)性質(zhì)
制備方法

110-91-8

1103738-17-5

1103738-19-7
以嗎啉和(3aS,5R,6S,6aS)-6-羥基-2,2-二甲基四氫呋喃[2,3-d][1,3]二氧雜環(huán)戊烯-5-羧酸為原料,合成((3aS,5R,6S,6aS)-6-羥基-2,2-二甲基四氫呋喃并[2,3-d][1,3]二氧雜環(huán)戊烯-5-基)(嗎啉代)甲酮的一般步驟如下:將(3aS,5R,6S,6aS)-6-羥基-2,2-二甲基四氫呋喃[2,3-d][1,3]二氧雜環(huán)戊烯-5-羧酸(5.0g,24.5mmol)溶于四氫呋喃(THF,100mL)中,加入TBTU(11.8g,1.5當(dāng)量)和N-甲基嗎啉(NMM,4.1mL,1.5當(dāng)量),混合物在20℃下攪拌30分鐘。隨后加入嗎啉(3.2mL,1.5當(dāng)量),反應(yīng)混合物在20℃下繼續(xù)攪拌6小時(shí)。反應(yīng)完成后,過濾除去固體,濾餅用THF(10mL)洗滌。合并有機(jī)相,減壓濃縮,殘余物通過硅膠柱色譜法(洗脫劑:己烷/乙酸乙酯,1:4至4:1)純化,得到4.3g白色固體產(chǎn)物,收率64%。產(chǎn)物經(jīng)1H NMR(CDCl3)表征,δ6.02(d,J=3.2Hz,1H),5.11(br s,1H),4.62(d,J=3.2Hz,1H),4.58(d,J=3.2Hz,1H),3.9-3.5(m,8H),1.51(s,3H),1.35(s,3H)。
參考文獻(xiàn):
[1] Patent: US2009/30198, 2009, A1. Location in patent: Page/Page column 8
[2] Patent: US2010/16422, 2010, A1. Location in patent: Page/Page column 4
[3] Patent: EP2332947, 2011, A1. Location in patent: Page/Page column 6-7
[4] Patent: EP2661256, 2018, B1. Location in patent: Paragraph 0091
[5] Patent: CN106892948, 2017, A. Location in patent: Paragraph 0195; 0196; 0197; 0198
報(bào)價(jià)日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價(jià)格 |
2025/05/22 | XW02110373819703 | ((3AS,5R,6S,6AS)-6-羥基-2,2-二甲基四氫呋喃并[2,3-D] [1,3]二氧雜環(huán)戊烯-5-基)(嗎啉代)甲酮 | 1103738-19-7 | 1G | 34元 |
2024/11/08 | XW02110373819702 | ((3AS,5R,6S,6AS)-6-羥基-2,2-二甲基四氫呋喃并[2,3-D] [1,3]二氧雜環(huán)戊烯-5-基)(嗎啉代)甲酮 | 1103738-19-7 | 250MG | 48.4元 |
2024/11/08 | XW02110373819701 | ((3AS,5R,6S,6AS)-6-羥基-2,2-二甲基四氫呋喃并[2,3-D] [1,3]二氧雜環(huán)戊烯-5-基)(嗎啉代)甲酮 | 1103738-19-7 | 100MG | 23.1元 |