CAS: 136725-55-8; (R)-(-)-3-Fluoropyrrolidine Hydrochloride

(R)-1-Boc-3-氟吡咯烷置于盐酸体系中,用 1,4-二氧六环,二氯甲烷 用作溶剂,化学反应 1.0H,以95.6%的收率获得3-(R)-氟吡咯烷(Hcl)
参考文献:一种卤素取代的拉曲替尼化合物
标题:一种卤素取代的拉曲替尼化合物
摘要:本发明涉及一种卤素取代的拉曲替尼化合物,包括放射性卤素原子或非放射性卤素原子标记的拉曲替尼硫酸氢盐化合物.所述的化合物包括结构式如下的化合物:(R,S)‑3‑18/19F‑larotrectinib或(R,R)‑3‑18/19F‑larotrectinib硫酸氢盐化合物,消旋‑3‑18/19F‑larotrectinib硫酸氢盐化合物,或类氟代羟基吡咯烷化合物,或类氟代羟基哌啶烷化合物.与现有技术相比,本发明研发出了新型的trk Pet探针,合成工艺路线简短,产物分离纯化方便,放化得率好,产物纯度(包括放射化学纯度)高.

专利信息

专利号:WO-2025087822-A1
优先权日:2023-10-23
标 题 :New process for the preparation of (3r)-fluoropyrrolidine hydrochloride
发明人：ENGL PASCAL STEPHAN; HILDBRAND STEFAN; MOESSNER CHRISTIAN; STOECKLI MARKUS; STUTZ ALFRED
权利人:HOFFMANN LA ROCHE; HOFFMANN LA ROCHE
摘要:The present invention relates to a new process for the preparation of (3R)-3-fluoropyrrolidine hydrochloride or an acceptable salts thereof via a N-Boc-(3S)-3-hydroxypyrrolidine intermediate. The process is suitable for the synthesis of N-Boc-(3S)-3- hydroxypyrrolidine at technical scale in high, not less than 99.85%-a/a optical purity and a purity of not less than 99.8%-a/a. The high quality N-Boc-(3S)-3-hydroxypyrrolidine can be converted to (3R)-3-fluoropyrrolidine hydrochloride exhibiting an optical purity of not less than 99.95%-a/a and a purity of not less than 99.5%-a/a thus making it a suitable intermediate for manufacturing of pharmaceutical active compounds.

专利号:US-2025313551-A1
优先权日:2022-12-15
标题 :Process for the preparation of a quinazolinone derivative
发明人：DOTT PASCAL JEAN CLAUDE; FANTASIA SERENA MARIA; GUILLEMOT-PLASS MAUD; KALDRE DAINIS; LARI GIACOMO MARCO; MODOLO-CHELLAT ISABELLE GEORGETTE HUGUETTE; SEDELMEIER JOERG MATHIAS; TROKOWSKI SEBASTIAN
权利人:HOFFMANN LA ROCHE
摘要:The present invention relates to a new process for the preparation of (3R)—N-[2-cyano-4-fluoro-3-(3-methyl-4-oxo-quinazolin-6-yl)oxy-phenyl]-3-fluoro-pyrrolidine-1-sulfonamide, as well as to a novel intermediate useful for the synthesis of said compound at large scale.

专利号:US-2022267331-A1
优先权日:2019-06-05
标题 :Dopamine-b-hydroxylase inhibitors
发明人：KISS LASZLO; BELIAEV ALEXANDER; ROSSI TINO; PALMA NUNO; SOARES DA SILVA PATRÃ?CIO; PINTO RUI; CARDONA FRANCISCO
权利人:BIAL PORTELA & CA SA
摘要:This invention relates to: (a) compounds of formula I (with R1 to R5 and A as defined herein) and pharmaceutically acceptable salts or solvates thereof that are useful as dopamine-β-hydroxylase inhibitors; (b) pharmaceutical compositions comprising such compounds, salts or solvates; (c) the use of such compounds, salts or solvates in therapy; (d) therapeutic methods of treatment using such compounds, salts or solvates; and (e) processes and intermediates useful for the synthesis of such compounds.

专利号:US-9856241-B2
优先权日:2013-07-03
标 题:Substituted benzofuranyl and benzoxazolyl compounds and uses thereof
发明人：BALOGLU ERKAN; SHACHAM SHARON; SENAPEDIS WILLIAM; MCCAULEY DILARA; LANDESMAN YOSEF; GOLAN GALI; KALID ORI; SHECHTER SHARON
权利人:KARYOPHARM THERAPEUTICS INC
摘要:The invention generally relates to substituted benzofuranyl and substituted benzoxazolyl compounds, and more particularly to a compound represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of Structural Formula (A), or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders.