专利号:US-3972945-A 优先权日:1974-12-23 标 题:Process for the selective synthesis of salicylaldehydes 发明人:ALBRIGHT CHARLES F 权利人:GARRETT CORP 摘要:The classical Reimer-Tiemann reaction for the synthesis of phenolic aldehydes has been modified from an aqueous to a non-aqueous system to provide an improved route for the formation of salicylaldehydes and, preferably, 3-substituted salicylaldehydes, e.g. 3-fluorosalicylaldehyde. Heretofore, compounds such as 3-substituted salicylaldehydes have proven to be extremely difficult to prepare in other than small laboratory quantities from the corresponding ortho-substituted phenol, since, in the final salicylaldehyde, each position ortho to the hydroxyl group contains substitution. In particular, with respect to 3-fluorosalicylaldehyde, one of the positions is occupied by the strongly electronegative fluorine atom so that the principal reaction product in the aqueous Reimer-Tiemann reaction has always been the para-isomer (3-fluoro-4-hydroxy-benzaldehyde), only negligible quantities of the desired ortho-isomer being obtained. In the process of the present invention, o-fluorophenol is caused to react with sodium hydroxide and chloroform in a hydrocarbon diluent (preferably benzene), maintaining the reaction under essentially anhydrous conditions by taking up the water of reaction with excess sodium hydroxide. It is necessary that an aprotic solvent, such as N,N-dimethylformamide, be employed as a catalyst. The use of boron oxide, while not absolutely necessary to the reaction, has been found to be advantageous in that the reaction proceeds more smoothly if the phenoxyboroxine is formed initially. The boron oxide also acts as a dehydrating agent and aids in removing the water of reaction. The preferential reaction product is the desired 3-fluorosalicylaldehyde, no paraisomer having been found. After hydrolysis and neutralization, the 3-fluorosalicylaldehyde can be recovered by azeotropic distillation along with a substantial quantity of unreacted o-fluorophenol which can be purified for recycle in subsequent preparations.
专利号:US-6414180-B1 优先权日:1998-03-04 标 题:Synthesis of chiral β-amino acids 发明人:COLSON PIERRE-JEAN; AWASTHI ALOK K; NAGARAJAN SRINIVASAN R 权利人:SEARLE & CO 摘要:The invention herein is directed to a process for the preparation of chiral beta-amino acids and esters of the formulawherein X and Y are the same or different halo groups, R2 is H or lower alkyl and isomers and pharmaceutically acceptable salts thereof.
专利号:US-10851070-B2 优先权日:2017-11-13 标 题 :Processes for the resolution of benzodiazepin-2-one and benzoazepin-2-one derivatives 发明人:HAGUE ANDREW; RONSHEIM MATTHEW 权利人:ENANTA PHARM INC; ENATA PHARMACEUTICALS INC 摘要:The present invention relates to processes and intermediates useful in the preparation of biologically active molecules, especially in the synthesis of Respiratory Syncytial Virus (RSV) inhibitors. The present invention also relates to processes and intermediates for the preparation of compounds of Formula (I-0) and Formula (I):
专利号:WO-2024121335-A1 优先权日:2022-12-07 标题:Synthesis of sulfoximine compounds having a stereogenic sulfur atom 发明人:WILLIAMS SIMON; SMITS HELMARS 权利人:SYNGENTA CROP PROTECTION AG 摘要:A process for the preparation of compound of formula (I) which process comprises: (A) stereoselectively oxidizing a sulfanyl compound of formula (II) followed by (B) stereospecific imination of a sulfinyl compound of formula (III) is disclosed wherein the substituents are as defined in claim 1.
专利号:EP-2524910-A1 优先权日:2011-05-17 标题 :Process for the resolution of aminobutyramide 发明人:BOESTEN WILHELMUS HUBERTUS JOSEPH; BOONEN JOZEF JOHANNES CATHERINA JACOBUS; WOESTENBORGHS PIERRE LOUIS 权利人:DSM IP ASSETS BV 摘要:The present invention relates to a process for the resolution of Schiff bases of racemic ( R,S )-2-aminobutyramide to give optically pure ( S )-2-aminobutyramide, an intermediate in the synthesis of levetiracetam.
专利号:US-6730787-B1 优先权日:1998-12-04 标题 :2,4Dioxo-5-arylidenimino-1,3-pyrimidines 发明人:KRUTIKOV VIKTOR I; ASHKINAZI RIMMA I 权利人:VIROMAX LLC 摘要:The invention relates to medicine, and more specifically to pharmacology, and in particular to synthetic biologically active derivatives of pyrimidine, and it is designated mainly for use as antiviral, immune-stimulating, antichlamydial, antituberculous, psychodepressant, analgesic, and hepatoprotective remedies. Besides that, these compounds may be used for treating malignant neoplasms, and also in veterinary. The objective of the invention is obtaining new chemical substances possessing pronounced biological activity of wide range. The proposed objective is achieved by synthesis of 2,4-dioxo-5-arylidenimino-1,3-pyrimidines of the general formulawhere R is chosen out of group H, OH, alkoxyl, dialkylamino, benzo, dibenzo, or 3,4-dioxolano General method of producing the claimed compounds and example of synthesis, a list of 25 compounds synthesized and tested, results of identification, and data on wide comparative testing their biological properties and toxicity are presented.