192725-45-4
192725-45-4 結(jié)構(gòu)式
基本信息
(2S,3S,5S)-2-(2,6-二甲基苯氧乙?；?氨基-3-羥基-5-(叔丁氧羰基)氨基-1,6-二苯基己烷
tert-Butyl ((2S,4S,5S)-5-(2-(2,6-dimethylphenoxy)acetamido)-4-hydroxy-1,6-diphenylhexan-2-yl)c
tert-Butyl ((2S,4S,5S)-5-(2-(2,6-dimethylphenoxy)acetamido)-4-hydroxy-1,6-diphenylhexan-2-yl)carb
tert-Butyl ((2S,4S,5S)-5-(2-(2,6-dimethylphenoxy)acetamido)-4-hydroxy-1,6-diphenylhexan-2-yl)carbamate
(2S,3S,5S)-2-(2,6-DIMETHYLPHENOXYACETYL)AMINO-3-HYDROXY-5-(T-BUTYLOXYCARBONYLAMINO)-1,6-DIPHENYLHEXANE
(2S,3S,5S)-2-(2,6-Dimethylphenoxyacetyl)amino-3-hydroxy-5-(tert-butoxycarbonyl)amino-1,6-diphenylhexane
tert-butyl N-[(2S,4S,5S)-5-[[2-(2,6-dimethylphenoxy)acetyl]amino]-4-hydroxy-1,6-diphenylhexan-2-yl]carbamate
N-[(1S,3S,4S)-4-[[2-(2,6-DiMethylphenoxy)acetyl]aMino]-3-hydroxy-5-phenyl-1-(phenylMethyl)pentyl]carbaMic Acid 1,1-DiMethylethyl Ester
Carbamic acid, N-[(1S,3S,4S)-4-[[2-(2,6-dimethylphenoxy)acetyl]amino]-3-hydroxy-5-phenyl-1-(phenylmethyl)pentyl]-, 1,1-dimethylethyl ester
物理化學(xué)性質(zhì)
制備方法
13335-71-2
![[(1S,3S,4S)-4-氨基-3-羥基-5-苯基-1-(苯甲基)戊基]-氨基甲酸叔丁酯](/CAS/GIF/144163-85-9.gif)
144163-85-9
192725-45-4
實(shí)施例18. (2S,3S,5S)-2-(2,6-二甲基苯氧乙?；?氨基-3-羥基-5-(叔丁氧羰基)氨基-1,6-二苯基己烷的制備：在室溫下，將(1S,3S,4S)-1-芐基-4-氨基-3-羥基-5-苯基戊基氨基甲酸叔丁酯（38.5 mg, 0.1 mmol）、2,6-二甲基苯氧基乙酸（18.9 mg, 1.05當(dāng)量）、1-(3-二甲基氨基丙基)-3-乙基碳二亞胺鹽酸鹽（29.7 mg, 1.5當(dāng)量）和1-羥基苯并三唑（20.4 mg, 1.5當(dāng)量）溶于N,N-二甲基甲酰胺（1 mL）中，攪拌4分鐘。隨后，向反應(yīng)混合物中加入N-甲基嗎啉（27.5 μL, 2.5當(dāng)量），繼續(xù)攪拌16小時(shí)。反應(yīng)完成后，用飽和碳酸氫鈉溶液淬滅反應(yīng)，用乙酸乙酯萃取。有機(jī)相用10%檸檬酸溶液洗滌，無(wú)水硫酸鈉干燥，減壓濃縮。通過(guò)硅膠柱色譜（3%甲醇/二氯甲烷）純化，得到白色固體產(chǎn)物（240 mg, 76.7%收率）。1H NMR (300 MHz, DMSO-D6) δ ppm: 1.31 (s, 9H), 1.39-1.55 (m, 2H), 2.14 (s, 6H), 2.61 (d, J = 6.99 Hz, 2H), 2.80 (d, J = 7.35 Hz, 2H), 3.61-3.70 (m, 1H), 3.84 (m, 1H), 4.00-4.11 (m, 2H), 4.20-4.38 (m, 1H), 4.99 (d, 1H), 6.66 (d, J = 9.19 Hz, 1H), 6.88-7.28 (m, 13H), 7.43 (d, J = 9.56 Hz, 1H); MS m/z 547.4 (M + H)+。
參考文獻(xiàn)：
[1] Patent: EP1170289, 2002, A2. Location in patent: Page 41
[2] Patent: WO2008/27932, 2008, A2. Location in patent: Page/Page column 101
[3] Bioorganic and Medicinal Chemistry Letters, 2002, vol. 12, # 21, p. 3101 - 3103
[4] Letters in Organic Chemistry, 2018, vol. 15, # 2, p. 87 - 91