专利号:US-2024294462-A1 优先权日:2023-02-15 标题:Method for the Synthesis of Ionizable Lipids Using a Doubly Alkylated Intermediate 发明人:SAADATI FARIBA; TRAN HUY; CIUFOLINI MARCO; ATMURI N D PRASAD 权利人:NANOVATION THERAPEUTICS INC 摘要:Provided herein is a method for the preparation of ionizable, cationic amino lipids using a doubly alkylated nucleophilic intermediate to produce a ketone. The ketone, or a corresponding alcohol, is subjected to one or more synthesis steps to add an ionizable moiety thereto. The method can be advantageously employed for the synthesis of unsymmetrical analogues of the above lipids that would be considerably more difficult to make by alternative strategies. The method can also be used to prepare symmetrical ionizable, cationic amino lipids with fewer steps and/or with the use of fewer hazardous chemicals than known synthesis methods.
专利号:US-4424159-A 优先权日:1978-05-26 标 题:Process for the synthesis of the hydroxyacetyl side-chain of steroids of the pregnane type, novel 21-hydroxy-20-oxo-17α-pregnane compounds and pharmaceutical preparations containing them 发明人:BIOLLAZ MICHEL 权利人:CIBA GEIGY CORP 摘要:The present invention relates to a novel general process for synthesizing a α- or β-oriented hydroxyacetyl side chain of steroids of the pregnane type, which comprises treating a corresponding steroid carbaldehyde in succession with formaldehyde dimethylmercaptal-S-oxide in the form of an alkali metal salt thereof, and with a strongly acid hydrolysing agent. n Preferred final products are compounds of the formula ##STR1## wherein n is 1 or 2, R 2 represents methyl or difluoromethyl, and R 1 represents hydroxymethyl, methoxymethyl, acetoxymethyl or hydrogen, and, if n is 2 and/or R 2 is difluoromethyl, R 1 also represents methyl. These compounds act as agonists or antagonists of natural steroid hormones. The antigestagenic 19,21-dihydroxy-17α-pregn-4-ene-3,20-dione and its 6,7-dehydro derivatives and diacetates are of particular interest.
专利号:US-4221915-A 优先权日:1977-03-11 标题:Process for preparing thiophene derivatives and thiophene derivatives obtained thereby 发明人:KONDO KIYOSHI; TSUNEMOTO DAIEI; FUJISAWA TAMOTSU 权利人:SAGAMI CHEM RES 摘要:Process for the preparation of a series of thiophene derivatives, from which 2-thiopheneacetic acid derivatives can easily be prepared, in high yields and selectivity by using substituted or unsubstituted thiophenes as the starting materials by easy operations. 2-Thiopheneacetic acid derivatives are very useful compounds as the chemical modifier of penicillin and cephalosporin. Novel compounds, i.e. α-arylthio-2-thiopheneacetic acids are also disclosed. These compounds are useful as the intermediates of the synthesis of 2-thiopheneacetic acids.
专利号:US-4742052-A 优先权日:1981-07-15 标题:Antibacterial β-lactam compounds 发明人:SUNAGAWA MAKOTO; MATSUMURA HARUKI; INOUE TAKAAKI; ENOMOTO MASAO 权利人:SUMITOMO PHARMA 摘要:Novel beta -lactam compounds classified into penem compounds, a process for preparing the same and use of such beta -lactam compounds are disclosed. These beta -lactam compounds exhibit excellent antimicrobial activities useful as pharmaceuticals or they are important intermediates for the synthesis of compounds having antimicrobial activities.
专利号:US-5659021-A 优先权日:1987-03-13 标 题 :Chiral glycerol derivatives 发明人:ABUSHANAB ELIE 权利人:RHODE ISLAND EDUCATION 摘要:Enantiomerically pure glycerol derivatives, e.g. S-1,2-O-isopropylidene, S-1,2-O-benzylidene, and R-1,2-O-dibenzyl glycerol, have been prepared from 1,2R-O-protected erythritols in high yields. The latter compounds are easily obtained from erythorbic acid and are useful building blocks in the synthesis of a host of optically active compounds having biological activity.
专利号:CA-2615490-A1 优先权日:2005-07-18 标题:Stereoselective synthesis of 3,4-disubstituted cyclopentanones and related compounds
摘要:Yoshikai, N.; Rayner, C. M.; Graham, M. A., Science of Synthesis Knowledge Updates, (2020) 2, 90. 摘要:Ishii, A., Science of Synthesis Knowledge Updates, (2016) 2, 351. 摘要:Ishii, A., Science of Synthesis Knowledge Updates, (2016) 2, 352. 摘要:Lattanzi, A., Science of Synthesis: Stereoselective Synthesis, (2011) 3, 1006. 摘要:Kaneda, K.; Mitsudome, T., Science of Synthesis: Catalytic Reduction in Organic Synthesis, (2017) 1, 344.