WO2025247057 - PREPARATION METHOD FOR CHIRAL R- OR S-3-METHYLMORPHOLINE
National phase entry is expected:
Publication Number
WO/2025/247057
Publication Date
04.12.2025
International Application No.
PCT/CN2025/096412
International Filing Date
21.05.2025
Title **
[English]
PREPARATION METHOD FOR CHIRAL R- OR S-3-METHYLMORPHOLINE
[French]
PROCÉDÉ DE PRÉPARATION DE R- OU S-3-MÉTHYLMORPHOLINE CHIRALE
[Chinese]
一种手性R或S的3-甲基吗啉的制备方法
Applicants **
SHANGHAI BALMXY PHARMACEUTIC CO., LTD
Inventors
YUAN, Xinkang
ZHAI, Zhiyang
HUANG, Shaolin
GUO, Pengfei
WANG, Di
ZHANG, Han
FU, Yongmei
Priority Data
202410698951.4
31.05.2024
CN
Application details
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International Searching Authority |
CNIPA
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| Recordal of a Change of the Applicant's Name/Address |
Change of Applicant's Name and Address
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| Type of Assignment |
The Standard Agent's Assignment
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| Applicant's Legal Status |
Legal Entity
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| Entry into National Phase under |
Chapter I
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| Patent Delivery |
Send the Letters Patent by Courier
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Quotation for National Phase entry
| Country | Stages | Total | |
|---|---|---|---|
| China | Filing, Examination, Granting | 1692 | |
| EPO | Filing, Examination, Granting | 11551 | |
| Japan | Filing, Examination, Granting | 2122 | |
| South Korea | Filing, Examination, Granting | 2066 | |
| USA | Filing, Examination, Granting | 4740 |

Total:
22,171
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Abstract[English]
Disclosed in the present invention is a preparation method for chiral R- or S-3-methylmorpholine. Chiral S- or R-propylene oxide is used as a starting material to react with Boc ethanolamine under the action of a Lewis acid, and then a chiral morpholine compound is obtained by means of a Mitsunobu reaction for ring closing. The preparation method of the present invention has shortened steps and enhanced total yield, thereby efficiently reducing the unit cost.[French]
La présente invention concerne un procédé de préparation de R- ou S-3-méthylmorpholine chirale. L'oxyde de S- ou R-propylène chiral est utilisé en tant que matériau de départ pour réagir avec la Boc éthanolamine sous l'action d'un acide de Lewis, puis un composé morpholine chirale est obtenu au moyen d'une réaction de Mitsunobu pour la fermeture de cycle. Le procédé de préparation de la présente invention présente des étapes raccourcies et un rendement total amélioré, ce qui permet de réduire efficacement le coût unitaire.[Chinese]
本发明公开了一种手性R或S的3-甲基吗啉的制备方法,以手性S或R环氧丙烷为原料,使其在路易斯酸作用下与Boc乙醇胺反应,然后经过光延反应关环,得到手性吗啉化合物。本发明的制备方法缩短了步骤,总收率提高,使得单位成本得到有效降低。