CAS: 1195-45-5; 4-Fluorophenylisocyanate

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对氟苯甲酸置于羟胺,N,N-二异丙基乙胺,对硝基苯磺酰氯体系中,用 四氢呋喃,水,乙腈 用作溶剂,化学反应 17.0H,反应生成异氰酸对氟苯基酯
参考文献:N-甲基咪唑催化异羟肟酸通过洛森重排合成氨基甲酸酯
标题:N-甲基咪唑催化异羟肟酸通过洛森重排合成氨基甲酸酯
摘要:报道了一种有效的,一锅法,N-甲基咪唑 (Nmi) 通过 Lossen 重排加速合成芳香族和脂肪族氨基甲酸酯的方法.Nmi 是将异氰酸酯中间体转化为氨基甲酸酯的催化剂.此外,芳基磺酰氯与 Nmi 组合的效用最大限度地减少了在序列过程中经常观测到的异羟肟酸酯-异氰酸酯二聚体的形成.在目前的条件下,降低温度也是可能的,从而实现温和的协议.
Doi:10.1021/ol303424B

专利信息

专利号:US-8710261-B2
优先权日:2005-02-22
标 题:5-phenyl-pentanoic acid derivatives as matrix metalloproteinase inhibitors for the treatment of asthma and other diseases
发明人：PALLE VENKATA P; SATTIGERI VISWAJANANI JITENDRA; KHERA MANOJ KUMAR; VOLETI SREEDHARA RAO; RAY ABHIJIT; DASTIDAR SUNANDA G
权利人:PALLE VENKATA P; SATTIGERI VISWAJANANI JITENDRA; KHERA MANOJ KUMAR; VOLETI SREEDHARA RAO; RAY ABHIJIT; DASTIDAR SUNANDA G; RANBAXY LAB LTD
摘要:The present invention relates to Compounds having the structure of Formula I: wherein n is an integer from 1 to 5; R 1 is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, aralkyl, alkoxy, aryloxy, alkenyloxy or alkynyloxy; R 2 is alkenyl, allcynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, NR 4 R 5 , —NHC(â•?Y)R 4 , —NHC(â•?Y)NR 5 R χ , —NHC(â•?O)OR 4 , —NHSO 2 R 4 , C(â•?Y)NR 4 R 5 , C(â•?O)OR 6 [wherein Y is oxygen or sulphur], OR 5 , —O(Câ•?O)NR 4 R 5 , O-acyl, S(O) m R 4 , —SO 2 N(R 4 ) 2 , cyano, amidino or guanidino [wherein R 4 is alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, aralkyl, heteroarylalkyl, heterocyclylalkyl or cycloalkylalkyl and m is an integer 0-2; R 5 is hydrogen or R 4 ; R x is R 4 or —SO 2 N(R 4 ) 2 and R 6 is hydrogen, alkyl, cycloalkyl, aralkyl, heteroarylalkyl, heterocyclylalkyl or cycloalkylalkyl]; R 3 is hydrogen, fluorine, alkyl, cycloalkylalkyl or aralkyl; A is OH, OR 4 , —OC(â•?O)NR 4 R 5 , O-acyl, NH 2 , NR 4 R 5 , —NHC(â•?Y)R 4 , —NHC(â•?Y)NR 5 R x , —NHC(â•?O)OR 4 , —NHSO 2 R 4 , and to processes for the synthesis of the same. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterize by over-expression and over-activation of an matrix metalloproteinase, using the compounds.

专利号:US-2008300251-A1
优先权日:2005-09-05
标 题 :Derivatives of 3-Azabicyclo[3.1.0] Hexane as Dipeptidyl Peptidase-IV Inhibitors
发明人：SATTIGERI JITENDRA A; ANDAPPAN MURUGAIAH M S; KISHORE KAUSHAL; SETHI SACHIN; KANDALKAR SACHIN RAMESH; PAL CHANCHAL KUMAR; MAHAJAN DIPAK C; AHMED SHAHADAT; PARKALE SANTHOSH SADASHIV; SRINIVASAN T; SHARMA LALIMA; BANSAL VINAY S; CHUGH ANITA; DAVIS JOSEPH ALEXANAND
权利人:SATTIGERI JITENDRA A; ANDAPPAN MURUGAIAH M S; KISHORE KAUSHAL; SETHI SACHIN; KANDALKAR SACHIN RAMESH; PAL CHANCHAL KUMAR; MAHAJAN DIPAK C; AHMED SHAHADAT; PARKALE SANTHOSH SADASHIV; SRINIVASAN T; SHARMA LALIMA; BANSAL VINAY S; CHUGH ANITA; DAVIS JOSEPH ALEXANAND
摘要:The present invention relates to novel 3-azabicyclo[3.1.0]hexane derivatives as dipeptidyl peptidase-IV inhibitors and the processes for the synthesis of the said compounds. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating diabetes, especially type 2 diabetes, as well as prediabetes, diabetic dyslipidemia, metabolic acidosis, ketosis, satiety disorders, and obesity. These inhibitors can also be used to treat conditions manifested by a variety of metabolic, neurological, anti-inflammatory, and autoimmune disorders like inflammatory disease, multiple sclerosis, rheumatoid arthritis; viral, cancer and gastrointestinal disorders. The compounds of this invention can also be used for treatment of infertility arising due to polycystic ovary syndrome.

专利号:US-4341898-A
优先权日:1981-05-18
标题:Synthesis of isocyanates from nitroalkanes
发明人：MILLIGAN BARTON; PINSCHMIDT JR ROBERT K
权利人:AIR PROD & CHEM
摘要:A process for the preparation of aromatic isocyanates from nitroalkanes. A nitromethyl aromatic compound of the general formula: wherein R and R1 represent hydrogen, halogen, a C1-C5 alkyl radical, a C1-C4 alkoxy radical, nitro, isocyanato, an alkoxycarbonylamino, or nitromethyl radical, with R and R1 being the same or different, is heated in the presence of an effective amount of a Lewis acid or Bronsted acid substance to effect a dehydrogenation-isomerization reaction to yield an aromatic isocyanate of the general formula: The product of the reaction may be recovered as the aromatic isocyanate or the alcohol adduct, a carbamate.

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-9676783-B2
优先权日:2008-10-22
标 题:Method of treatment using substituted pyrazolo[1,5-A] pyrimidine compounds
发明人：HAAS JULIA; ANDREWS STEVEN W; JIANG YUTONG; ZHANG GAN
权利人:ARRAY BIOPHARMA INC
摘要:Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.

专利号:US-2022281888-A1
优先权日:2019-09-25
标题:Bicyclic carboxylates as modulators of transporters and uses thereof
发明人：SANDANAYAKA VINCENT; GORECZNY GREGORY
权利人:NIROGY THERAPEUTICS INC
摘要:The present invention generally relates to the field of transporter modulators, e.g., monocarboxylate transporter inhibitors, and more particularly to new bicyclic enone carboxylate compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with monocarboxylate transporter activity such as in treating cancer and other neoplastic disorders, tissue and organ transplant rejection.