6052-68-2

基本信息
L-色氨酸EP雜質(zhì)H
色氨酸雜質(zhì)H (EP)
N-乙酰色氨酸EP雜質(zhì)H
2,3,4,9-四氫-1H-beta-咔啉-3-甲酸
2,3,4,9-四氫-1H-BETA-咔啉-3-羧酸
2,3,4,9-四氫-1H-吡咯并[3,4-B]吲哚-3-羧酸
2,3,4,9-四氫-1H-吡啶并[3,4-B]吲哚-3-羧酸
DL-Tpi-OH
AKOS BC-1280
AKOS BBS-00007515
Tryptophan EP Impurity H
N-Acetyltryptophan EP Impurity H
TETRAHYDRO-BETA-CARBOLINECARBOXYLICACID
(S)-(-)-2 3 4 9-TETRAHYDRO-1H-PYRIDO &
TETRAHYDRO-BETA-CARBOLINE-3-CARBOXYLICACID
1,2,3,4-TETRAHYDRONORHARMANE-3-CARBOXYLIC ACID
物理化學(xué)性質(zhì)
制備方法

50-00-0

73-22-3

6052-68-2
以甲醛和L-色氨酸為原料合成2,3,4,9-四氫-1H-吡啶并[3,4-b]吲哚-3-羧酸的一般步驟如下:首先,將1-丙磺酸(817 mg,4 mmol)與2.5 M NaOH溶液(1.6 mL)混合,室溫下攪拌直至混合物變澄清。隨后,向混合物中加入37%福爾馬林(4.87 mL)。將反應(yīng)混合物在室溫下攪拌2小時,然后回流3小時。反應(yīng)完成后,用2 M HCl溶液中和至pH 5。析出的沉淀經(jīng)過濾后,依次用水和甲醇洗滌,最后在真空下干燥,得到目標(biāo)產(chǎn)物2,3,4,9-四氫-1H-吡啶并[3,4-b]吲哚-3-羧酸。該步驟的產(chǎn)率為99%,產(chǎn)物為無色固體,熔點為302.2-304.6℃。質(zhì)譜(FAB)分析顯示m/z 217(M+1, 100%)。
參考文獻(xiàn):
[1] European Journal of Medicinal Chemistry, 2011, vol. 46, # 2, p. 636 - 646
[2] Acta chemica Scandinavica (Copenhagen, Denmark : 1989), 1994, vol. 48, # 5, p. 434 - 438
[3] Patent: CN106432235, 2017, A. Location in patent: Paragraph 0217; 0218
[4] Patent: US2013/178629, 2013, A1. Location in patent: Paragraph 0109
[5] Molecules, 2010, vol. 15, # 11, p. 7775 - 7791