CAS: 2349386-89-4; Eidd-2801;Molnupiravir

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参考文献:5'-异丁酰基-N4-羟基胞苷的制备方法
标题:5'-异丁酰基-N4-羟基胞苷的制备方法
摘要:本发明揭示了一种具有预防和治疗包括新冠(Covid‑19)在内的多种病毒感染作用的5'‑异丁酰基‑n4‑羟基胞苷的制备方法,其制备步骤包括:以d‑核糖和胞嘧啶为起始原料,分别通过叉丙酮保护,酰化和羟胺化反应,所得化合物经过缩合和水解反应制得式i化合物5'‑异丁酰基‑n4‑羟基胞苷.该制备方法原料易得,工艺简洁,经济环保,适合工业化生产.

专利信息

专利号:US-11672829-B2
优先权日:2015-09-10
标 题:Genetically engineered coronavirus-specific effector cells for in situ synthesis of antiviral proteins
发明人：BHATNAGAR PARIJAT; SSEMADAALI MARVIN A
权利人:STANFORD RES INST INT
摘要:An example genetically engineered effector cell comprises an exogenous polynucleotide sequence that includes a receptor element, an actuator element, and an effector element. The receptor element encodes a chimeric antigen receptor (CAR) comprising an extracellular antigen binding domain operably linked to a transmembrane domain, and an intracellular signaling domain, wherein the extracellular antigen binding domain recognizes an antigen on a surface of a Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2)-infected cell. The actuator element encodes a transcription factor binding site that upregulates synthesis of an antiviral protein. The effector element encodes the antiviral protein operably linked to a signal peptide, wherein, in response to the antigen binding domain of the CAR binding to the antigen of SARS-CoV-2-infected cell, the engineered effector cell is configured to activate and, to synthesize and secrete the antiviral protein.

专利号:WO-2022208508-A1
优先权日:2021-03-31
标 题:Scalable two step synthesis of molnupiravir
发明人：DATLA ANUPAMA; NAGRE PRASHANT; TAMORE JAGDISH; PRABHU MANOJKUMAR SADANAND; TRIVIKRAM SREENATH; KADAM SACHIN VASANT; DEGAONKAR GAJANAN SUBHASH; MURALIDHARAN KRISHNA; RUPRAJ NARAIN
权利人:FERMENTA BIOTECH LTD
摘要:The present invention provides a scalable two-step synthesis of molnupiravir. The reaction sequence involves the use of commercially easily available cytidine (1), and molnupiravir is formed through direct hydroxy amination of the cytidine followed by esterification of the primary alcohol without protecting dihydroxy groups (vicinal diols) i.e. without formation of acetonide.

专利号:WO-2022168106-A1
优先权日:2021-02-06
标题:Chemo-enzymatic process for synthesis of molnupiravir
发明人：DATLA ANUPAMA; NAGRE PRASHANT; TAMORE JAGDISH; PRABHU MANOJKUMAR SADANAND; TRIVIKRAM SREENATH
权利人:FERMENTA BIOTECH LTD
摘要:Disclosed herein is a process for synthesis of Molnupiravir from cytidine of using a lipase for esterification reaction. The process comprises of reacting compound of formula II with acetone in presence of sulphuric acid to obtain compound of formula III; enzymatically converting compound of Formula III to compound of Formula IV, and Hydroxyaminating Formula IV using Hydroxyl amine sulphate or hydrochloride followed by deprotection to obtain compound of formula I

专利号:WO-2023021530-A1
优先权日:2021-08-18
标题:Improved short process for synthesis of molnupiravir
发明人：DATLA ANUPAMA; NAGRE PRASHANT; TAMORE JAGDISH; PRABHU MANOJKUMAR SADANAND; TRIVIKRAM SREENATH; DEGAONKAR GAJANAN SUBHASH; WADHAVANE SACHIN GOVIND; SHIRSATH AMOL; PAWAR PRASAD
权利人:FERMENTA BIOTECH LTD
摘要:The present invention discloses an economical and improved, short process for synthesis of Molnupiravir from cytidine. The process of the present invention provides a novel intermediate N-Hydroxy Cytidine isobutyryl ester (13) which can be enzymatically converted to Molnupiravir in good yield and purity.

专利号:WO-2022168107-A1
优先权日:2021-02-06
标题 :Enzymatic synthesis of molnupiravir intermediate
发明人：DATLA ANUPAMA; NAGRE PRASHANT; TAMORE JAGDISH; PRABHU MANOJKUMAR SADANAND; TRIVIKRAM SREENATH; ASHAR TRUPTI KRISHNAKANT; JAIN RINA; KADAM SACHIN VASANT
权利人:FERMENTA BIOTECH LTD
摘要:Disclosed herein is the enzymatic process for synthesis of Molnupiravir intermediate, 5'-isobutylester of cytidine acetonide. The process employs cytidine acetonide as starting material to prepare 5'-isobutylester of cytidine acetonide. The esterification of cytidine acetonide is carried out using Enzyme CAL B expressed in Pichia pastoris. The present invention further discloses processes for preparation of O-Isobutyl acetone oxime.

专利号:WO-2023118363-A1
优先权日:2021-12-22
标题:Method for the synthesis of a carbonyl-functionalised adduct
发明人：GODEHARD SIMON P; PELZER ALEXANDER
权利人:BRAIN Biotech AG
摘要:The invention relates to a method for the synthesis of a carbonyl-functionalised adduct.