69-74-9 (盐酸阿糖胞苷,Cytarabine hydrochloride)

盐酸阿糖胞苷;阿糖胞苷盐酸盐;阿糖胞甙;胞嘧啶阿拉伯糖苷盐酸盐;盐酸阿糖胞嘧啶;1-beta-D-阿拉伯呋喃糖基-4-氨基-2(1H)-嘧啶酮盐酸盐;阿糖胞嘧啶;氧氨嘧啶-B-D-阿拉伯醇苷盐酸盐;安西他宾;胞嘧啶 β-D-呋喃阿拉伯糖苷盐酸盐;1-(β-D-呋喃阿拉伯糖苷)-胞嘧啶盐酸盐;1-Β-D-阿拉伯呋喃糖基-4-氨基-2(1H)-嘧啶酮盐酸盐;阿拉伯糖胞嘧啶盐酸盐;阿糖胞嘧啶盐酸盐;胞嘧啶-BETA-D-阿拉伯呋喃糖 盐酸盐;1-(β-D-呋喃阿拉伯糖苷)­胞嘧啶 盐酸盐;Ara-C 盐酸盐;胞嘧啶阿拉伯糖苷 盐酸盐;阿拉伯糖胞嘧啶 盐酸盐;阿糖胞嘧啶 盐酸盐;阿糖胞苷 盐酸盐;

cytosine arabinoside hydrochloride;1-beta-d-arabinofuranosyl-cytosinhydrochloride;1-beta-d-arabinofuranosyl-cytosinmonohydrochloride;4-amino-1-beta-d-arabinofuranosyl-2(1h)-pyrimidinonmonohydrochloride;4-Amino-1-D-Arabinofuranosyl-2(1H)-PyrimidinoneHydrochloride;ac1075;arabinofuranosylcytosinehydrochloride;arabinosylcytosinehydrochloride;Cytosine β-D-arabinofuranoside hydrochloride;1-beta-D-Arabinofuranosylcytosine hydrochloride;1-β-D-Arabinofuranosylcytosine hydrochloride;4-Amino-1-((2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)-tetrahydrofuran-2-yl)pyrimidin-2(1H)-one hydrochloride;Cytarabine;Cytarabine hydrochloride;CYTARABINE HYDROCHLORIDE USP 26;Ara-C hydrochloride;4-Amino-1-[(2S,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one;hydrochloride;Cytosine-1-beta-D-arabinofuranoside hydrochloride;MLS000028466;UNII-33K3DB6591;CHEMBL1256472;MFCD00012839;SCHEMBL67288;Cytarabin hydrochloride;EU-0100316;1beta-D-Arabinofuranosylcytosine hydrochloride;1-beta-D-arabinofuranosylcytosinhydrochlorid;Cytosine, 1-beta-D-arabinofuranosyl-, hydrochloride;MLS001148147;1beta-D-Arabinofuranosylcytosine monohydrochloride;C 6645;SMR000058432;AKOS015960559;AKOS015995277;2(1H)-Pyrimidinone, 4-amino-1-.beta.-D-arabinofuranosyl-, hydrochloride;CYTARABINE HYDROCHLORIDE [WHO-DD];Alexan hydrochloride;CCRIS 4774;Cytosine, 1-beta-D-arabinofuranosyl-, monohydrochloride;CYTARABINE HYDROCHLORIDE (SEEALSO CYTARABINE 147-94-4);LS-1589;Spongocytidine hydrochloride;Cytosine beta -D-arabinofuranoside hydrochloride;4-amino-1-[(2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]pyrimidin-2(1H)-one hydrochloride;2(1H)-Pyrimidinone,4-amino-1-b-D-arabinofuranosyl-,hydrochloride (1:1);Opera_ID_1542;Arabinofuranosylcytosine hydrochloride;SR-01000075773;AC-32195;Tox21_500316;2(1H)-Pyrimidinone, 4-amino-1-beta-D-arabinofuranosyl-, monohydrochloride;Q27256279;Cylocide;Arabinosylcytosine hydrochloride;Aracytin hydrochloride;AKOS015896936;Cytosine beta-D-arabinofuranoside hydrochloride, crystalline;Arabinocytidine hydrochloride; Arabinosylcytosine hydrochloride; Ara-C hydrochloride;s5582;NCGC00261001-01;C9-H13-N3-O5.Cl-H;Aracytidine hydrochloride;KCURWTAZOZXKSJ-JBMRGDGGSA-N;2(1H)-Pyrimidinone, 4-amino-1-.beta.-D-arabinofuranosyl-, monohydrochloride;AI3-52344;4-amino-1-((2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)pyrimidin-2(1H)-one hydrochloride;SR-01000075773-1;Arabinosyl cytosine hydrochloride;CCG-221620;NSC 63878;69-74-9 (HCL);BA164338;DTXCID104891;29363-79-9;CAS-69-74-9;NSC-63878;1-.BETA.-D-ARABINOFURANOSYLCYTOSINE MONOHYDROCHLORIDE;NCGC00254321-01;Cytosar hydrochloride;Arabitin hydrochloride;EINECS 200-713-9;Cytarabine hydrochloride [USAN];Cytosine, 1beta-D-arabinofuranosyl-, monohydrochloride;Cytarabine HCl;Tox21_300488;C9H13N3O5.HCl;4-Amino-1-((2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)pyrimidin-2(1H)-one hydrochloride(1:x);33K3DB6591;Cytarabine hydrochloride (USAN);C9H13N3O5.ClH;AMY15521;Cytosine beta-D-arabinofuranoside hydrochloride;1-b-D-Arabinofuranosylcytosine hydrochloride;LP00316;1-beta-D-Arabinofuranosylcytosine monohydrochloride;D03637;Cytosine, 1-.beta.-D-arabinofuranosyl-, hydrochloride;NCGC00093762-01;HY-13605A;Cytosine-beta-D-arabinofuranose hydrochloride;4-Amino-1-((2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)pyrimidin-2(1H)-onehydrochloride(1:x);DTXSID5024891;A51105;4-amino-1-[(2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one;hydrochloride;Cytosine, 1-beta-D-arabinofuranosyl-, monhydrochloride;AC-11705;Cytarabine (hydrochloride);U-19920A;AC 1075;69-74-9;MLS002207299;NS00076327;1-(b-D-Arabinofuranosyl)cytosine hydrochloride;1-(beta-d-arabino-furanosyl)-cytosine hydrochloride;Arabinocytidine hydrochloride;DB-025611;GLXC-15916;SCH-900242;Cytarabine hydrochloride - Bio-X trade mark;NA05780;Cytosine ?-D-arabinofuranoside hydrochloride;1-(?-D-Arabinofuranosyl)cytosine hydrochloride;Ara-C.hydrochloride;NSC63878;Spongocytidine-hydrochloride;4-Amino-1-beta-d-arabinofuranosyl-2(1H)-pyrimidinone hydrochloride;4-AMINO-1-BETA-D-ARABINOFURANOSYL-2(1H)-PYRIMIDINONE MONOHYDROCHLORIDE;200-713-9;Ara-C HCl;Cytosine ?-D-arabinofuranoside hydrochloride;Ara-C.hydrochloride;Cytosine Arabinosine Hydrochloride;

MFCD00012839

KCURWTAZOZXKSJ-JBMRGDGGSA-N

1S/C9H13N3O5.ClH/c10-5-1-2-12(9(16)11-5)8-7(15)6(14)4(3-13)17-8;/h1-2,4,6-8,13-15H,3H2,(H2,10,11,16);1H/t4-,6-,7+,8-;/m1./s1

Cl.O1[C@H](CO)[C@H]([C@@H]([C@@H]1N1C(N=C(C=C1)N)=O)O)O

200-713-9

2942000000

医药生物化工中间体。

方法一、5'-胞苷-磷酸(5'-CMP)为原料 胞嘧啶核苷盐酸盐的制备 5'-胞苷-磷酸100g悬浮于800ml蒸馏水中,加入约50ml浓氨水,调节pH值为8-9,不溶物可过滤除去,稀释至1L后加入氢氧化镧凝胶1L,升温至90℃搅拌水解(水解过程中可通过对氢氧化镧凝胶的电泳分析来确定反应终点),当电泳纸上5'-胞苷-磷酸斑点消失并有胞嘧啶核苷的斑点出现后(约需25h)反应结束,离心得上清液,沉淀用6L蒸馏水洗两次后离心,将洗液与上清液混合。减压浓缩,浓缩中可过滤除去不溶物,浓缩至约0.2L后停止,冷却,用6mol/L盐酸调节pH为2.5-3,即有白色结晶析出,加100m1 95%乙醇,冰箱冷却过夜后过滤,用稀醇及无水乙醇洗涤,得产品。 5'-胞苷-磷酸[氨水,氢氧化镧]→[pH8-9, 90℃, 25h]胞嘧啶核苷盐酸盐 胞嘧啶阿拉伯糖苷的制备 300ml三氯氧磷先预冷20min,加预冷的蒸馏水30ml,有盐酸气体放出,5min后,将反应液置冰盐浴30min。加入乙酸乙酯2L及胞嘧啶核苷盐酸盐40g,热水浴中80℃回流,时间约为40-50min。将反应液倾入4L蒸馏水中,50℃减压蒸出乙酸乙酯。浓缩液用****溶液调pH为3-3.5,加浓氨水,80℃水解10min,过滤除去不溶物。滤液调pH为2.5-3,上活性炭柱,分别用pH为3的蒸馏水和60℃的50%乙醇-1%氨水洗脱,将洗脱液浓缩至20ml左右,调pH为3,加乙醇冷却结晶,过滤,得产品。 胞嘧啶核苷盐酸盐[三氯氧化磷,乙酸乙酯,水]→[0-80℃, 40-50min]2, 2'-氧桥-3',5'-二乙酰基胞嘧啶核苷盐酸盐[氨水]→[80℃,10min]阿糖胞苷 阿糖胞苷盐酸盐的制备 将阿糖胞苷22g加入2%盐酸-甲醇440ml及甲醇220ml,50℃水浴加热溶解,活性炭脱色半小时后过滤,浓缩,冰箱冷却过夜,过滤得粗品,用30倍甲醇重结晶得纯品。 阿糖胞苷[盐酸,甲醇]→[50℃, 30min]阿糖胞苷盐酸盐 方法二、以葡萄糖酸钙为原料 D-阿拉伯糖的制备 投料为葡萄糖酸钙(m):硫酸铁(m):无水乙酸钡 (m):水(V):过氧化氢(V)=1:0.077:0.14:13:1.2-1.3。葡萄糖酸钙加水加热溶解后,加入事先配好的乙酸钡溶液和硫酸铁溶液的混合液,搅拌升温至95℃,过滤除去不溶物,滤液加一半用量的过氧化氢于40-56℃反应30min,静置30min,再于40℃加入剩余的过氧化氢反应30min,加入草酸过滤除去草酸钙,滤液在50℃以下真空浓缩,加无水甲醇溶解结晶,过滤得粗品,甲醇重结晶得纯品。 葡萄糖酸钙[乙酸钡,硫酸铁,过氧化氢]→[40-56℃,1.5 h]D-阿拉伯糖 2-氨基-D-阿拉伯糖-噁唑啉的制备 投料比为D-阿拉伯糖(m):氰胺 (m):氨水(V):甲醇(V)=1:0.56:0.3-0.35:3-4。将氰胺溶于甲醇中配成15%-20%的溶液,加D-阿拉伯糖和氨水,搅拌下缓慢加热至内温为51-62℃ (约1h),保温反应30min后搅拌放置2h,再放置过夜,过滤得产品。 D-阿拉伯糖[氰胺,氨水,甲醇]→[57-62℃,30min]2-氨基-D-阿拉伯糖-噁唑啉 阿糖胞苷盐酸盐的制备 投料比为丙炔氰(m):2-氨基-D-阿拉伯糖-噁唑啉(m):二甲基乙酰胺(m):氨水(1mol/L,V)=1:3.25:10:40-50。将2-氨基-D-阿拉伯糖-噁唑啉和二甲基乙酰胺混合,搅拌下冷却至5℃,滴加丙炔氰和少量二甲基乙酰胺的混合液,控制滴加速度使温度不超过10℃,滴完后于25℃搅拌反应30min,过滤,滤液加氨水于60℃搅拌10min,60℃以下减压蒸馏除水,浓缩液用盐酸甲醇溶液(3%-5%)调pH至4,冷却使析出结晶,过滤得粗品,用20-50倍的甲醇精制,加活性炭脱色,得阿糖胞苷盐酸盐。 2-氨基-D-阿拉伯糖-噁唑啉[丙炔氰,二甲基乙酰胺]→[25℃, 30min]环胞苷[氨水,盐酸-甲醇溶液]→[pH4]阿糖胞苷盐酸盐。