CAS: 3024-72-4; 3,4-Dichlorobenzoyl Chloride

上下游产品

CAS号51-44-5 3,4-二氯苯甲酸 | CAS号10286-79-0 3,4-dichloro-N-... | CAS号110623-30-8 5-(3,4-dichloro... | CAS号2039-83-0 3,4-二氯苯乙烯 | CAS号18094-90-1 3,4-dichloro-N-... | CAS号28394-58-3 3,4-二氯苯甲酸乙酯 | CAS号27891-18-5 N-butan-2-yl-3,... | CAS号2448-04-6 Benzamide,3,4-d... | CAS号20555-91-3 3,4-二氯碘苯 | CAS号328-84-7 3,4-二氯三氟甲苯 | CAS号28036-91-1 3,4-二氯苯甲酰肼

3,4-二氯苯甲酸置于氯化亚砜体系中,用91%的收率获得3,4-二氯苯甲酰氯
参考文献:Synthesis And Structure-Activity Relationship Studies Of N-Monosubstituted Aroylthioureas As Urease Inhibitors
标题:Synthesis And Structure-Activity Relationship Studies Of N-Monosubstituted Aroylthioureas As Urease Inhibitors
摘要:背景: 硫脲是一种经典的尿素酶抑制剂,通常用作阳性对照,许多n,N'-二取代硫脲已被确定为尿素酶抑制剂.然而,由于空间位阻,N,N'-二取代硫脲基团无法像硫脲那样结合尿素酶.相反,具有微小硫脲基团的n-单取代硫脲理论上可以像硫脲一样结合到活性口袋中. 目标: 设计并合成了一系列n-单取代芳酰硫脲,用于评估其作为尿素酶抑制剂的效果. 方法: 通过吲哚酚法确定尿素酶抑制作用,并利用量化对数剂量-概率函数的计算机化线性回归分析计算ic50值.通过表面等离子共振(spr)和基于从迈克尔斯-门特金动力学导出的混合型抑制模型的非线性回归分析估计动力学参数. 结果: 化合物b2,B11和b19以混合机制可逆地抑制尿素酶,并对无细胞尿素酶和完整细胞中的尿素酶表现出极佳的效力,其ic50值分别比阳性对照乙酰羟羟肟酸低90至450倍和5至50倍.最有效的化合物b11对无细胞尿素酶显示出ic50值为0.060 +/-0.004μm,其与尿素结合位点的结合具有非常低的kd值(0.420+/-0.003Nm)和非常长的停留时间(6.7分钟).化合物b11还被证明对哺乳动物细胞具有非常低的细胞毒性. 结论: 结果表明,N-单取代芳酰硫脲如预期地结合到尿素酶的活性位点,并代表了一类新的尿素酶抑制剂,可用于开发针对含尿素酶病原体引起的感染的潜在治疗药物.
Doi:10.2174/1573406416999200818152440

专利信息

专利号:US-6608196-B2
优先权日:2001-05-03
标题 :Process for solid supported synthesis of pyruvate-derived compounds
发明人：WANG BING; JANAGANI SATYANARAYANA; CALLAWAY WYETH B; SESSLER JONATHAN L
权利人:GALILEO PHARMACEUTICALS INC
摘要:Provided are processes for synthesizing structurally diverse pyruvate-derived compounds using a parallel approach on a solid phase support. Examples of such a solid phase support include resins which have also been used in solid phase peptide synthesis.

专利号:US-6191277-B1
优先权日:1998-04-29
标 题:Hydroxypropylamide peptidomimetics as inhibitors of aspartyl proteases
发明人：DOLLE III ROLAND ELLWOOD; CAVALLARO CULLEN LEE; HERPIN TIMOTHEE FELIX
权利人:PHARMACOPEIA INC
摘要:Compounds of Formula Iare disclosed as inhibitors having activity against the aspartyl proteases, plasmepsin and cathsepsin D. The compounds are useful for treatment of diseases such as malaria and Alzheimer's disease. In preferred compounds of Formula I, Y is a heterocycle, amide, sulfonamide or carbamate and Z is an acyl or a functionalized acyl. Intermediates in the solid phase synthesis of compounds of Formula I, in which compounds are attached to a solid phase support, are also disclosed.

专利号:US-8778958-B2
优先权日:2008-07-10
标题 :Synthesis of metabolically stable agents for alcohol and drug abuse
发明人：CASHMAN JOHN R
权利人:CASHMAN JOHN R
摘要:The disclosed opioid-related compounds and pharmaceutical compositions thereof, are useful in a variety of applications relating to the modulation of receptors and receptor signaling within and outside the nervous system. For example, the compounds and compositions are useful in methods for the treatment of addictions and other CNS-related disorders. The disclosed compounds can be delivered or administered to a mammal including humans, alone in the form of a pharmaceutically acceptable salt or hydrolysable precursor thereof, or in the form of a pharmaceutical composition, wherein a therapeutically effective amount of a compound is mixed with suitable carriers or excipients.

专利号:US-8481501-B2
优先权日:2004-05-28
标 题 :Synthesis of metabolically stable analgesics, pain medications and other agents
发明人：CASHMAN JOHN R; MACDOUGALL JAMES M
权利人:CASHMAN JOHN R; MACDOUGALL JAMES M; HUMAN BIOMOLECULAR RES INST
摘要:Disclosed are analgesic-related compositions and methods of using the compositions for modulation of analgesic receptor activity. The compositions and methods are useful for reducing pain, as well as for therapeutic intervention of addictions or other diseases or disorders amenable to treatment or prophylaxis by modulation of analgesic receptor signaling.

专利号:WO-9700244-A1
优先权日:1995-06-19
标题 :Process for parallel synthesis of a non-peptide library
发明人：FRITZ JAMES E; KALDOR STEPHEN W
权利人:LILLY CO ELI; FRITZ JAMES E; KALDOR STEPHEN W
摘要:A process for the sequential preparation of a library of compounds having pharmaceutical usage. The process involves the sequential mixing of solution phase reagents, followed by scavenging of excess unreacted reagents with solid phase scavenging agents. The process is highly iterative and applicable for producing various ureas, thiureas, amides, carbonates and tertiary amines.

专利号:US-2005234244-A1
优先权日:2004-04-20
标题:Synthesis of COX-2 and FAAH inhibitors
发明人：BARTOLINI WILMIN; CALI BRIAN M; CHEN BARBARA; CHIEN YUEH-TYNG; CURRIE MARK G; MILNE G T; PEARSON JAMES P; TALLEY JOHN J; ZIMMERMAN CRAIG
权利人:BARTOLINI WILMIN; CALI BRIAN M; CHEN BARBARA; CHIEN YUEH-TYNG; CURRIE MARK G; MILNE G T; PEARSON JAMES P; TALLEY JOHN J; ZIMMERMAN CRAIG
摘要:Methods for preparing indoles that are useful COX-2 inhibitors and intermediates useful in such methods are described.