公开(公告)号：US20240246820A1

公开(公告)日：2024-07-25

申请号：US18625907

申请日：2024-04-03

Applicant: Fudan University

Inventor： Fener CHEN ,  Minjie LIU ,  Li WAN ,  Yajiao ZHANG ,  Dang CHENG

IPC: C01B21/46 ,  B01D1/00 ,  B01D5/00

CPC classification number: C01B21/46 ,  B01D1/0082 ,  B01D5/006 ,  B01D5/0075

Abstract: A method for on-line continuous recovery of excess nitric acid in nitration reaction is provided. Nitration reaction liquid and nitrogen gas are simultaneously conveyed to a mixer, mixed and transferred to a temperature-controlled corrosion-resistant column for on-line continuous evaporation, where the nitration reaction liquid enters the temperature-controlled corrosion-resistant column from a top end, and the waste gas and excess nitric acid are discharged from a top port of the temperature-controlled corrosion-resistant column, and nitric acid is recovered. The nitric acid-free liquid is discharged from a bottom end of the temperature-controlled corrosion-resistant column by a pump.

公开(公告)号：US20220267253A1

公开(公告)日：2022-08-25

申请号：US17741112

申请日：2022-05-10

Applicant: Fudan University

Inventor： Fener CHEN ,  Minjie LIU ,  Meifen JIANG ,  Dang CHENG ,  Chao YU ,  Huashan HUANG

IPC: C07C227/12 ,  B01J19/00

Abstract: A full continuous-flow preparation method of L-carnitine, including: mixing chlorine gas and a diketene solution via a first micromixer followed by transportation to a first microchannel reactor for continuous chlorination and esterification reaction to obtain 4-chloroacetoacetate; feeding the 4-chloroacetoacetate and a reductase to a second micromixer and a second microchannel reactor in sequence for continuous catalytic reaction to obtain (R)-4-chloro-3-hydroxybutyrate; simultaneously transporting the (R)-4-chloro-3-hydroxybutyrate and a trimethylamine solution to a third micromixer and a third microchannel reactor for continuous substitution and hydrolysis reaction; and subjecting the reaction mixture to desalination and concentration to obtain the L-carnitine.

公开(公告)号：US20220090151A1

公开(公告)日：2022-03-24

申请号：US17545963

申请日：2021-12-08

Applicant: Fudan University

Inventor： Fener CHEN ,  Yuan TAO ,  Zedu HUANG ,  Dang CHENG ,  Ge MENG

IPC: C12P13/00

Abstract: An enzyme-catalyzed method of synthesizing (2S, 3R)-2-substituted aminomethyl-3-hydroxybutyrate, including: preparing engineered bacteria containing a carbonyl reductase SsCR-encoding gene; preparing a resting cell suspension of the engineered bacteria; preparing a culture containing carbonyl reductase; and mixing the culture containing carbonyl reductase with substrate 2-substituted aminomethyl-3-one butyrate, glucose dehydrogenase, a cosolvent, glucose and a cofactor followed by asymmetric carbonyl reduction to obtain (2S, 3R)-2-substituted aminomethyl-3-hydroxybutyrate. The amino acid sequence of the carbonyl reductase is shown in SEQ ID NO.1.

公开(公告)号：US20210394149A1

公开(公告)日：2021-12-23

申请号：US17467060

申请日：2021-09-03

Applicant: Fudan University

Inventor： Fener CHEN ,  Meifen JIANG ,  Dang CHENG ,  Minjie LIU ,  Huashan HUANG

IPC: B01J19/00 ,  C07D239/42

Abstract: Disclosed herein relates to pharmaceutical engineering, and more particularly to a micro reaction system and a method for preparing 2-methyl-4-amino-5-cyanopyrimidine using the same. An acetamidine hydrochloride solution and an (dimethylaminomethylene)malononitrile solution are separately pumped into the micro reaction system including a micromixer and an agitating microchannel reactor in communication at the same time for a continuous condensation-cyclization reaction to obtain 2-methyl-4-amino-5-cyanopyrimidine.

公开(公告)号：US20210355516A1

公开(公告)日：2021-11-18

申请号：US17038081

申请日：2020-09-30

Applicant: Fudan University

Inventor： Fener CHEN ,  Kejie ZHU ,  Zedu HUANG ,  Dang CHENG ,  Jiaqi WANG ,  Yuan TAO

IPC: C12P17/04 ,  C12N9/02 ,  C12N1/20 ,  C12N15/70

Abstract: An enzyme-catalyzed synthesis of (1S,5R)-bicyclolactone. A first genetically-engineered bacterium containing Baeyer-Villiger monooxygenase gene and a second genetically-engineered bacterium containing glucose dehydrogenase gene are constructed and then suspended with culture medium to prepare a first suspension and a second suspension, respectively. The first and second suspensions are centrifuged to respectively produce a first supernatant containing Baeyer-Villiger monooxygenase and a second supernatant containing glucose dehydrogenase, which are mixed. The mixed supernatant is then mixed with a raceme of a substituted bicyclo[3.2.0]-hept-2-en-6-one, a solvent, a hydrogen donor and a cofactor to perform an asymmetric Baeyer-Villiger oxidation to produce the (1S,5R)-bicyclolactone, where an amino acid sequence of the Baeyer-Villiger monooxygenase is shown in SEQ ID NO:1.

公开(公告)号：US20210040109A1

公开(公告)日：2021-02-11

申请号：US16986200

申请日：2020-08-05

Applicant: Fudan University

Inventor： Fener CHEN ,  Yali SANG ,  Chunlin ZHUANG

IPC: C07D495/04 ,  A61P31/18

Abstract: A biphenyl-containing diarylpyrimido compound of formula (I), which is prepared by reacting a 4-chloropyrimidine derivative with a biphenyl derivative in a solvent in the presence of a base. A pharmaceutically-acceptable salt of the compound (I) and a pharmaceutical composition containing the compound (I) or a pharmaceutically-acceptable salt thereof are also provided.

公开(公告)号：US20180339974A1

公开(公告)日：2018-11-29

申请号：US15871049

申请日：2018-01-14

Applicant: FUDAN UNIVERSITY

Inventor： Fener CHEN ,  Guanxin HUANG ,  Ge MENG ,  Minjie LIU ,  Yan WU ,  Dang CHENG ,  Zedu HUANG ,  Haihui PENG ,  Fangjun XIONG

IPC: C07D319/06 ,  C07B41/12 ,  C07B47/00

CPC classification number: C07D319/06 ,  C07B41/12 ,  C07B47/00

Abstract: The present disclosure belongs to the technical field of organic synthesis and particularly relates to a preparation method for 2-((4R,6S)-6-bromomethyl-2-oxo-1,3-dioxane-4-yl)acetate. The 2-((4R,6S)-6-bromomethyl-2-oxo-1,3-dioxane-4-yl)acetate is a key chiral intermediate for preparation of statin antilipemic agents. In the present disclosure, the 2-((4R,6S)-6-bromomethyl-2-oxo-1,3-dioxane-4-yl)acetate is obtained by bromination and cyclization of 3-((substituted oxycarbonyl)oxy)-5-hexenoate as raw material with hypochlorite and bromide in an organic solvent in the presence of CO2. The method of the present disclosure has the advantages of readily available raw material, mild reaction conditions, easy operation, low cost, excellent atomic economy and less by-products, and is applicable to industrial production.

公开(公告)号：US20240018088A1

公开(公告)日：2024-01-18

申请号：US18361533

申请日：2023-07-28

Applicant: Fudan University

Inventor： Fener CHEN ,  Minjie LIU

IPC: C07C201/16

CPC classification number: C07C201/16

Abstract: A separation and purification method of 2-nitroethanol, including: (a) reacting paraformaldehyde with nitromethane in the presence of a base to obtain a mixture of 2-nitroethanol (I), 2-nitro-1,3-propanediol (II) and tris(hydroxymethyl) nitromethane (III); and (b) selecting an extraction solvent in which 2-nitroethanol (I), 2-nitro-1,3-propanediol (II) and tris(hydroxymethyl) nitromethane (III) are different in solubility; adding the extraction solvent to the mixture followed by extraction, separation, and vacuum concentration to obtain the 2-nitroethanol (I).

公开(公告)号：US20230183260A1

公开(公告)日：2023-06-15

申请号：US18166906

申请日：2023-02-09

Applicant: Fudan University

Inventor： Fener CHEN ,  Dang CHENG ,  Jiale WU ,  Meifen JIANG ,  Li WAN ,  Jiaqi WANG

IPC: C07D495/04 ,  B01J19/00

CPC classification number: C07D495/04 ,  B01J19/0093 ,  B01J2219/00867 ,  B01J2219/00033

Abstract: A full continuous-flow preparation method of (+)-biotin, including: subjecting a cyclic anhydride and a chiral biphenyl propylene glycol to asymmetric ring-opening reaction to produce a first intermediate, which undergoes selective reduction with a borohydride and cyclization with an inorganic mineral acid to produce (3aS, 6aR)-lactone; subjecting the (3aS, 6aR)-lactone and a sulfenylating reagent to sulfenylation to produce (3aS, 6aR)-thiolactone, which undergoes Fukuyama coupling with a zinc reagent in the presence of a palladium catalyst and elimination reaction in the presence of an inorganic mineral acid to produce an alkenyl valerate compound; subjecting the alkenyl valerate compound to reduction in the presence of a Pd/C catalyst to produce a valerate ester, which undergoes hydrolysis to produce a valeric acid salt; and subjecting the valeric acid salt to debenzylation in the presence of an inorganic mineral acid to produce the target product (+)-biotin.

公开(公告)号：US20210403449A1

公开(公告)日：2021-12-30

申请号：US17468447

申请日：2021-09-07

Applicant: Fudan University

Inventor： Fener CHEN ,  Chunlin ZHUANG ,  Li DING

IPC: C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D401/14 ,  C07D239/48 ,  A61P31/18

Abstract: This application provides a biphenyl diaryl pyrimidine derivative with an aromatic heterocyclic structure, a pharmaceutically-acceptable salt, a stereoisomer, a hydrate and a solvate thereof, where the biphenyl diaryl pyrimidine derivative is shown in formula (I). This application also provides a pharmaceutical composition containing the biphenyl diaryl pyrimidine derivative, or a pharmaceutically-acceptable salt, a stereoisomer, a hydrate and a solvate thereof, and a pharmaceutically-acceptable carrier. This application further provides a method of treating AIDS by administering a therapeutically effective amount of the pharmaceutical composition to a patient in need.