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1. WO2020228170 - CATALYST-FREE SYNTHESIS METHOD FOR LACTAM DERIVATIVE

Publication Number WO/2020/228170
Publication Date 19.11.2020
International Application No. PCT/CN2019/102066
International Filing Date 22.08.2019
IPC
C07D 207/267 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
207Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
18having one double bond between ring members or between a ring member and a non-ring member
22with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
24Oxygen or sulfur atoms
262-Pyrrolidones
263with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
267with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to the ring nitrogen atom
C07D 211/76 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
68having one double bond between ring members or between a ring member and a non-ring member
72with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
74Oxygen atoms
76attached in position 2 or 6
C07D 209/46 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02condensed with one carbocyclic ring
44Iso-indoles; Hydrogenated iso-indoles
46with an oxygen atom in position 1
C07D 409/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
409Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
02containing two hetero rings
04directly linked by a ring-member-to-ring- member bond
Applicants
  • 贵州大学 GUIZHOU UNIVERSITY [CN]/[CN]
Inventors
  • 杨松 YANG, Song
  • 李虎 LI, Hu
  • 吴红果 WU, Hongguo
Agents
  • 贵阳中新专利商标事务所 GUIYANG ZHONGXIN PATENT AND TRADEMARK OFFICE
Priority Data
201910404767.316.05.2019CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) CATALYST-FREE SYNTHESIS METHOD FOR LACTAM DERIVATIVE
(FR) PROCÉDÉ DE SYNTHÈSE SANS CATALYSEUR D'UN DÉRIVÉ DE LACTAME
(ZH) 一种无催化剂合成内酰胺衍生物的方法
Abstract
(EN)
Disclosed is a simple synthesis method for a lactam derivative. The method comprises: using formamide as an amine source and a hydrogen donor (hydrolyzed to produce formic acid), and keto acid as a raw material, and simply synthesizing the lactam derivative through a cycloamination reaction without a solvent or a catalyst. Compared with previous reports, the time required for the reaction is greatly reduced, the selectivity is significantly improved, the conversion rate of the keto acid derivative is greater than 99%, and the yield of the lactam derivative can reach 70-94%.
(FR)
La présente invention concerne un procédé de synthèse simple d’un dérivé de lactame. Le procédé consiste à : utiliser du formamide en tant que source d'amine et un donneur d'hydrogène (hydrolysé pour produire de l'acide formique) et un céto-acide en tant que matière première et synthétiser de manière simple le dérivé de lactame par une réaction de cycloamination sans solvant ni catalyseur. Par rapport aux rapports précédents, le temps requis pour la réaction est fortement réduit, la sélectivité est considérablement améliorée, le taux de conversion du dérivé céto-acide est supérieur à 99 % et le rendement en dérivé de lactame peut atteindre 70-94 %.
(ZH)
本发明公开了一种内酰胺衍生物的简易合成方法,包括:以甲酰胺为胺源和氢供体(水解产生甲酸),酮酸为原料,在无溶剂和催化剂的条件下,经成环胺化反应简易合成内酰胺衍生物。与先前报道相比,本反应所需时间大大缩短、选择性得到显著提高,酮酸类衍生物的转化率>99%,内酰胺衍生物产率可达到70~94%。
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