Maleic Dihydrazide置于三氯氧磷体系中,用78.7%的收率获得3,6-二氯哒嗪 参考文献:Synthesis And Herbicidal Evaluation Of 3-N-Substituted Amino-6-Benzyloxypyridazine Derivatives 标题:Synthesis And Herbicidal Evaluation Of 3-N-Substituted Amino-6-Benzyloxypyridazine Derivatives 摘要:A Variety Of 3‐n‐substituted Amino‐6‐benzyloxypyridazine Derivatives Were Designed And Synthesized In Satisfactory Yields. Their Structures Were Confirmed By Ir,1H‐NMR,And Elemental Analysis; Compound 5J Was Further Determined By X‐ray Diffraction Crystallography. Their Herbicidal Activities Were Evaluated Through Barnyard Grass And Rape Cup Tests In Laboratory Bioassays. Most Of The Title Compounds 5 Displayed Moderate Herbicidal Activities Against The Dicotyledonous Plant Brassica Campestris L. The Most Active Compounds In The Laboratory Were Also Evaluated In The Greenhouse. Doi:10.1002/jhet.1831
专利信息
专利号:WO-2024084491-A1 优先权日:2022-10-21 标题:Process for synthesis of res metirom and its intermediates thereof 发明人:MEHTA NILESH VIPINCHANDRA 权利人:MEHTA NILESH VIPINCHANDRA 摘要:The present invention discloses a process for synthesis of Res metirom and its intermediates thereof. More particularly, the invention discloses process for synthesis of a key intermediate, 6-(4-amino, 2,6-dichlorophenoxy)4- isopropylpyridazin-3(2H)-one, of Res metirom via novel intermediate compounds of formula A. Wherein, R is selected from methyl, ethyl and propyl.
专利号:US-9968612-B2 优先权日:2012-09-17 标题:Method of synthesizing thyroid hormone analogs and polymorphs thereof 发明人:TAUB REBECCA; REYNOLDS CHARLES H 权利人:MADRIGAL PHARMACEUTICALS INC 摘要:The disclosure describes methods of synthesis of pyridazinone compounds as thyroid hormone analogs and their prodrugs. Preferred methods according to the disclosure allow for large-scale preparation of pyridazinone compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of pyridazinone compounds in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of a pyridazinone compound. Further disclosed is a method for treating resistance to thyroid hormone in a subject having at least one TRβ mutation.
专利号:WO-2025128848-A1 优先权日:2023-12-12 标题:Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:HOUZE JONATHAN B; PANDYA BHAUMIK 权利人:VIGIL NEUROSCIENCE INC 摘要:The present disclosure provides compounds of Formula (I), useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 ('TREM2'). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula (I).
专利号:WO-0107415-A1 优先权日:1999-07-28 标 题 :Method of producing pyridazine-3,6-dicarboxylic acid esters 发明人:BESSARD YVES; CRETTAZ ROGER; BRIEDEN WALTER 权利人:LONZA AG; BESSARD YVES; CRETTAZ ROGER; BRIEDEN WALTER 摘要:The invention relates to a method of producing pyridazine-3,6-dicarboxylic acid esters of the general formula (I), wherein R represents C1-10 alkyl, C3-8 cycloalkyl or aryl-C1-4-alkyl, by reacting 3,6-dichloropyridazine with carbon monoxide and alcohols R-OH in the presence of palladium-phosphine complexes and bases. The invention also relates to novel pyridazine-3,6-dicarboxylic acid esters (I), wherein R represents C3-10 alkyl, C3-8 cycloalkyl or aryl-C<1-4>-alkyl. The pyridazine-3,6-dicarboxylic acid esters (I) are the potential intermediates for the synthesis of pharmaceutical active substances.
专利号:WO-0107416-A1 优先权日:1999-07-28 标题 :Method of producing pyridazine carboxylic acid derivatives 发明人:BESSARD YVES; CRETTAZ ROGER; EGGEL MICHAEL 权利人:LONZA AG; BESSARD YVES; CRETTAZ ROGER; EGGEL MICHAEL 摘要:The invention relates to a method of producing pyridazine carboxylic acid derivatives of the general formulae (Ia) or (Ib), wherein R<1> represents a group of the formula -OR<3> or -NR<4>R<5>, R<2> represents hydrogen, chlorine, a group of the formula -OR<6> or a group of the formula -NR<7>R<8>, R<3> represents C1-10 alkyl, C3-8 cycloalkyl or aryl-C1-4-alkyl, R<4> represents C1-10 alkyl, C3-8 cycloalkyl, optionally substituted aryl or aryl-C1-4-alkyl, R<5> represents hydrogen, C1-10 alkyl, C3-8 cycloalkyl, optionally substituted aryl or aryl-C1-4-alkyl and R<6> represents C1-10 alkyl, C3-8 cycloalkyl, aryl-C1-4-alkyl or an optionally substituted aromatic or heteroaromatic rest and R<7> and R<8> represent independently C1-10 alkyl, C3-8 cycloalkyl or aryl-C1-4-alkyl or together with the nitrogen atom form a saturated or aromatic heterocyclic ring. The inventive derivatives are obtained by reacting the corresponding 3-chloropyridazines or 3,6-dichloropyridazine with carbon monoxide and alcohols or amines H-R<1> in the presence of palladium-phosphin complexes and bases. The pyridazine carboxylic acid derivatives (Ia, Ib) are the intermediates for the synthesis of pharmaceutically active substances.
专利号:WO-2024256360-A1 优先权日:2023-06-12 标题 :Method and system for calculating mass flow and estimating sustainability metrics in chemical synthesis 发明人:HAENSEL HELMUT; WIRSING SARA; BATHE ANDREAS; DAUTH ALEXANDER; KUEHNE BENJAMIN; BECKER HEINRICH; HELL KERSTIN 权利人:MERCK PATENT GMBH 摘要:A method is disclosed that selects one or more experimental IDs from an electronic notebook. The method links the one or more experimental IDs to form an integrated process to synthesize a target material and estimate a plurality of process metrics wherein each of the plurality of process metrics corresponds to a respective experimental ID of the one or more experimental IDs. The method estimates an aggregate process metric corresponding to the integrated process. The aggregate process metric is a function of the estimated plurality of process metrics. The method provides a synthesis tree corresponding to the one or more experimental IDs and searches for similar reaction subprocesses for each of the experimental IDs to determine a plurality of similar experiments. The method also selects an alternative experimental ID for at least one of the one or more experimental IDs and updates the aggregate process metric in accordance with the alternative experimental ID.