RESUMO
An enantioselective Ni-catalyzed cross-coupling of N-hydroxyphthalimide esters with vinyl bromides is reported. The reaction proceeds under mild conditions and uses tetrakis(N,N-dimethylamino)ethylene as a terminal organic reductant. Good functional group tolerance is demonstrated, with over 20 examples of reactions that proceed with >90% ee.
Assuntos
Ésteres/química , Níquel/química , Ftalimidas/química , Compostos de Vinila/química , Catálise , Oxirredução , Estereoisomerismo , TemperaturaRESUMO
An asymmetric Ni-catalyzed reductive cross-coupling of (hetero)aryl iodides and benzylic chlorides has been developed to prepare enantioenriched 1,1-diarylalkanes. As part of these studies, a new chiral bioxazoline ligand, 4-heptyl-BiOX (L1), was developed in order to obtain products in synthetically useful yield and enantioselectivity. The reaction tolerates a variety of heterocyclic coupling partners, including pyridines, pyrimidines, indoles, and piperidines.
Assuntos
Alcanos/síntese química , Níquel/química , Alcanos/química , Catálise , Hidrocarbonetos Clorados/química , Hidrocarbonetos Iodados/química , Estrutura Molecular , Oxirredução , EstereoisomerismoAssuntos
Adenoma/complicações , Neoplasias das Glândulas Suprarrenais/diagnóstico , Cistadenoma Mucinoso/diagnóstico , Linfangioma/diagnóstico , Neoplasias Primárias Múltiplas , Neoplasias Pancreáticas/diagnóstico , Adenoma/diagnóstico , Idoso , Colangiopancreatografia por Ressonância Magnética , Diagnóstico Diferencial , Feminino , Humanos , Pessoa de Meia-Idade , Neoplasias Pancreáticas/complicações , Tomografia Computadorizada por Raios XRESUMO
A 39-year-old female presented to our hospital with diarrhea, vomiting, anemia, and hypoalbuminemia. Virtual enteroscopy was performed to evaluate the small bowel; we found annular stenoses at 89, 100, 116, 147, and 154 cm from the ligament of Treitz. Small bowel resection was performed, and annular ulcers were confirmed at 58, 71, 90, 130, 138, 218, and 225 cm from the ligament of Treitz. Clinical records and pathological examination failed to determine the cause of these ulcers, and we diagnosed chronic multiple ulcers of the small intestine. Thus, we believe that virtual enteroscopy can be beneficial in preoperatively diagnosing multiple ulcers and stenoses in the small bowel.
Assuntos
Colonografia Tomográfica Computadorizada/métodos , Enteropatias/diagnóstico , Intestino Delgado , Úlcera/diagnóstico , Adulto , Doença Crônica , Constrição Patológica/diagnóstico , Constrição Patológica/patologia , Feminino , Humanos , Enteropatias/patologia , Intestino Delgado/patologia , Úlcera/patologiaRESUMO
A 37-year-old woman was admitted with left upper quadrant pain. Imaging examinations revealed a cystic mass with a diameter of 70 mm near the tail of the pancreas. The mass had a distorted fascicular structure adjacent to the hilum of the spleen. On operation the distorted fascicular structure was revealed to be connective tissue including vessels. On histopathological examination, the mass was strongly suspected to be an accessory spleen because spleen-like stroma was recognized, in spite of degeneration due to infarction.
Assuntos
Baço/anormalidades , Esplenopatias/patologia , Anormalidade Torcional/patologia , Adulto , Feminino , HumanosRESUMO
5-Alkenyl or 5-alkynyl-4-anilinopyrimidines were prepared and evaluated for in vitro inhibition of EGFR/Her-2 kinase activity and the growth of tumor cell lines (BT474 and N87). Several of these compounds inhibited the growth of BT474 and N87 at concentrations below 200nM. Structure-activity relationship studies revealed a critical role for the 5-alkynyl moieties. The representative compound 19 exhibited significant antitumor potency in a mouse xenograft model.
Assuntos
Receptores ErbB/antagonistas & inibidores , Receptor ErbB-2/antagonistas & inibidores , Administração Oral , Animais , Química Farmacêutica/métodos , Desenho de Fármacos , Ensaios de Seleção de Medicamentos Antitumorais/métodos , Inibidores Enzimáticos/farmacologia , Receptores ErbB/química , Humanos , Concentração de Íons de Hidrogênio , Concentração Inibidora 50 , Camundongos , Microssomos Hepáticos/metabolismo , Modelos Químicos , Transplante de Neoplasias , Pirimidinas/química , Ratos , Receptor ErbB-2/química , Relação Estrutura-AtividadeRESUMO
A structure-activity relationship study of 4-anilinopyrimidines for dual EGFR/Her-2 inhibitor has resulted in the identification of 4-anilino-5-alkenyl or 5-alkynyl-6-methylpyrimidine derivatives that have exhibited effective inhibitory activity against both enzymes. The presence of 5-alkenyl or 5-alkynyl moiety bearing terminal hydrophilic group played important role for inhibition of these enzymes. Selected compounds in the series demonstrated some activity against Her-2 dependent cell line (BT474).
Assuntos
Receptores ErbB/antagonistas & inibidores , Pirimidinas/síntese química , Pirimidinas/farmacologia , Receptor ErbB-2/antagonistas & inibidores , Cristalografia por Raios X , Avaliação Pré-Clínica de Medicamentos , Receptores ErbB/química , Humanos , Modelos Moleculares , Relação Estrutura-AtividadeRESUMO
A 72-year-old man with cough and sputum showed esophageal wall thickening and pneumonia in chest computed tomography (CT) scan. Following endoscopy, we diagnosed reflux esophagitis and subscribed proton pump inhibitor. The esophageal lesion, however, was intractable. We diagnosed microscopic polyangiitis (MPA) because of vasculitis symptoms, cytoplasmic antineutrophil cytoplasmic antibodies (cANCA) in blood and no granulomatous change in the esophagus. We adopted pulse therapy of cyclophosphamide and oral prednisolone; the symptoms and esophageal lesion were markedly improved. We concluded that the esophageal lesion was an aspect of MPA. To our knowledge, this is the first report of esophageal involvement in MPA.