CAS: 477600-75-2; 3-((3R,4R)-4-Methyl-3-(Methyl(7H-Pyrrolo[2,3-D]Pyrimidin-4-yl)Amino)Piperidin-1-yl)-3-Oxopropanenitrile

上下游产品

N-甲基-N-((3R,4R)-4-甲基哌啶-3-基)-7H-吡咯并[2,3-D]嘧啶-4-胺 N-Methyl-N-((3R,4R)-4-Methylpiperidin-3-yl)-7H-Pyrrolo[2,3-D]Pyrimidin-4-Amine 477600-74-1
N-甲基-N-((3S,4S)-4-甲基哌啶-3-基)-7H-吡咯并[2,3-D]嘧啶-4-胺 Methyl(4-Methylpiperidin-3-yl)-(7H-Pyrrolo[2,3-D]Pyrimidin-4-yl)Amine 384336-73-6
(3R,4R)-Tert-Butyl 4-Methyl-3-(Methyl(7H-Pyrrolo[2,3-D]Pyrimidin-4-yl)Amino)Piperidine-1-Carboxylate 1450663-24-7
(3R,4R)-(1-苄基-4-甲基-哌啶-3-基)-甲基-(7H-吡咯并[2,3-D]嘧啶-4-基)-胺 N-((3R,4R)-1-Benzyl-4-Methylpiperidin-3-yl)-N-Methyl-7H-Pyrrolo[2,3-D]Pyrimidin-4-Amine 477600-73-0
托法替布相关杂质22 (1-Benzyl-4-Methyl-Piperidin-3-yl)-Methyl-(7H-Pyrrolo[2,3-D]Pyrimidin-4-yl)-Amine 384337-90-0
托法替尼杂质2 2-Chloro-N-Methyl-N-[(3R,4R)-4-Methylpiperidin-3-Yl]-7H-Pyrroio[2,3-D]Pyrimidin-4-Amine 1616760-97-4
2-Chloro-N-Methyl-N-[(3R,4R)-4-Methyl-1-(Triphenylmethyl)-3-Piperidinyl]-7H-Pyrrolo[2,3-D]Pyrimidin-4-Amine 1616760-96-3
托法替尼 Intb3 N-((3R,4R)-1-Benzyl-4-Methylpiperidin-3-yl)-N-Methyl-7-Tosyl-7H-Pyrrolo[2,3-D]Pyrimidin-4-Amine 923036-30-0
2-Chloro-N-Methyl-7-[(4-Methylphenyl)Sulfonyl]-N-[(3R,4R)-4-Methyl-1-(Triphenylmethyl)-3-Piperidinyl]-7H-Pyrrolo[2,3-D]Pyrimidin-4-Amine 1616760-94-1

4-氯-7H-吡咯并[2,3-D]嘧啶-7-羧酸叔丁酯置于盐酸,氢气,Potassium Carbonate,1-羟基苯并三唑,盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺,三乙胺体系中,用 甲醇,二氯甲烷,乙酸乙酯,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 17.0H,反应生成 托法替尼
参考文献:一种枸橼酸托法替尼的制备方法
标题:一种枸橼酸托法替尼的制备方法
摘要:本发明涉及一种枸橼酸托法替尼的制备方法,具体涉及以4‑氯‑7‑吡咯并[2,3‑d]嘧啶,(Boc)2O,(3R,4R)‑(1‑苄基‑4‑甲基哌啶‑3‑基)甲胺‑l‑二对甲苯甲酰酒石酸盐,Pd/c,氰基乙酸和枸橼酸为原料,经氨基保护反应,氨基化反应,脱苄基反应,缩合反应,脱保护反应和成盐反应六步高产率合成枸橼酸托法替尼.本合成路线提供了一种枸橼酸托法替尼的制备方法是一种高收率,低成本,易操作,适宜工业化的制备方法.

专利信息

专利号:US-8309716-B2
优先权日:2005-07-29
标题 :Pyrrolo[2,3-d]pyrimidine derivatives: their intermediates and synthesis
发明人：RUGGERI SALLY GUT; HAWKINS JOEL M; MAKOWSKI TERESA M; RUTHERFORD JENNIFER L; URBAN FRANK J
权利人:RUGGERI SALLY GUT; HAWKINS JOEL M; MAKOWSKI TERESA M; RUTHERFORD JENNIFER L; URBAN FRANK J; PFIZER
摘要:This invention relates to methods and intermediates useful for the synthesis of pyrrolo[2,3-d]pyrimidine compounds. Specifically novel synthetic methods and intermediates for the synthesis of 3-{(3R,4R)-4-methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino}-piperidin-1-yl)-3-oxo-propionitrile and its corresponding citrate salt are disclosed.

专利号:US-2025206743-A1
优先权日:2022-03-25
标 题:Tyk2 inhibitor synthesis and intermediates thereof
发明人：MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
权利人:TAKEDA PHARMACEUTICALS CO
摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

专利号:US-11827598-B1
优先权日:2022-07-15
标 题:Preparation method of tofacitinib citrate
发明人：HSU YAO-LUNG; HSIEH KUANG-CHAN; CHENG HUI-WEN; Yang zong-han
权利人:CHUNGHWA CHEMICAL SYNTHESIS & BIOTECH CO LTD
摘要:The present disclosure provides a preparation method of tofacitinib citrate, which comprises the following steps: passing an intermediate TOF-2 into hydrogen at a normal pressure in the presence of a catalyst to obtain an intermediate TOF-3; in the presence of a solvent and a base, under a reduced pressure of −490 mmHg to −760 mmHg, and at a temperature of 10° C. to 25° C., reacting TOF-3 with ethyl cyanoacetate to generate an intermediate TOF-4; heating and dissolving TOF-4 and citric acid in a solvent, and performing separation by cooling to obtain tofacitinib citrate. The present disclosure obtains tofacitinib citrate with high yield, high purity and low impurities by changing a gas flow rate and a reaction temperature and pressure of a hydrogenation reaction. Therefore, the preparation method is suitable for industrial production.

专利号:US-2025289827-A1
优先权日:2022-12-02
标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
发明人：YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
权利人:C4 THERAPEUTICS INC
摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.

专利号:US-9828380-B2
优先权日:2015-04-10
标题 :Efficient method for the preparation of tofacitinib citrate
发明人：BONANOMI JACOPO; DEFIORE STELLA; NOVO BARBARA
权利人:OLON SPA
摘要:Disclosed is a novel process for the synthesis of tofacitinib citrate on an industrial scale with high yields and purity starting with cis-(1-benzyl-4-methyl-piperidin-3-yl)methylamine bis-hydrochloride racemate (intermediate VIII), which comprises:n 1. Condensation between intermediates VII and VIII to give intermediate VI 2. Hydrogenation of intermediate VI to give intermediate V 3. Resolution of intermediate V to give intermediate IV with enantiomeric purity >99% 4. Release of intermediate IV in a basic medium to give intermediate III 5. N-acylation reaction of intermediate III to give II (tofacitinib) 6. Salification of intermediate II to give tofacitinib monocitrate (I)

专利号:US-11993606-B2
优先权日:2015-10-16
标题:Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
发明人：MOHAMED MOHAMED-ESLAM F; OTHMAN AHMED A; PANGAN AILEEN L; SONG IN-HO; KLÃœNDER BEN; VOSS JEFFREY W; PADLEY ROBERT J; CAMP HEIDI S
权利人:ABBVIE INC
摘要:The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and various spondyloarthritic conditions, including types of axial spondyloarthritis (axSpA)), kits, methods of synthesis, and products-by-process. In various aspects, provided are methods for treating active non-radiographic axSpA (nr-axSpA) and methods for treating active ankylosing spondylitis (AS).