Facile synthesis of sulfinate esters from aryl iodides via direct oxidation of thioesters.

A practical method to synthesize sulfinate esters from aryl iodides is disclosed. Direct oxidation of thioesters prepared by copper-catalyzed C-S formation of aryl iodides realized the efficient synthesis of sulfinate esters. Due to the good accessibility of aryl iodides, a wide variety of sulfinate esters were prepared from easily available starting materials such as carboxylic acids and anilines.

Facile synthesis of dibenzothiophene S-oxides from sulfinate esters.

An efficient method to prepare dibenzothiophene S-oxides is disclosed. Suzuki-Miyaura cross-coupling of 2-bromoaryl sulfinate esters with arylboronic acids selectively at the bromo group followed by electrophilic cyclization of the resulting sulfinate ester moiety provides diverse dibenzothiophene S-oxides. Further transformations including Pummerer-type C-H propargylation and aryne reactions realize to synthesize highly functionalized dibenzothiophene derivatives.

[A case of effective weekly paclitaxel administration for gastric cancer recurrence with carcinomatous pericarditis].

We reported a case of effective weekly paclitaxel administration for gastric cancer recurrence with carcinomatous pericarditis. A 69-year-old man underwent distal gastrectomy for gastric cancer in December 2001. However, he was re-admitted to the hospital for dyspnea in November 2002. A diagnosis of cardiac tamponade caused by gastric cancer relapse was made, and the patient was treated by weekly paclitaxel administration (90 mg/body) after drainage. It was effective in preventing reaccumulation of the pericardial effusion until his death 73 days after the diagnosis. It is thought that weekly paclitaxel administration can be a treatment for carcinomatous pericarditis.

[A case of peritoneal dissemination of postoperative primary duodenal cancer successfully treated by TS-1 therapy].

A 62-year-old man reported to our hospital with serious complaints of abdominal pain, vomiting, and weight loss. An endoscopic examination detected a type 2 tumor of the descending limb of the duodenum. With a diagnosis of adenocarcinoma based on the biopsy finding, the patient was subjected to surgery. Laparotomy revealed the presence of a duodenal tumor disseminating to the omentum at the site where the transverse colon is attached. Pancreatoduodenectomy and partial resection of the transverse colon were carried out. CT conducted 6 months after surgery did not show any signs of tumor recurrence; but one year later, extensive tumor dissemination was noted on the hepatic surface. Upon consultation with the patient, a regimen of 80 mg/day of TS-1 given for 4 weeks followed by 2 weeks of a drug-free period was initiated. Six months later, the growth of tumor became arrested, improving his QOL. Nine months later, the tumor growth was progressive and the patient died two years after operation. The patient could gain long-term survival after operation. The TS-1 regimen applied in the present case may constitute a therapeutic strategy to be considered for similar conditions in future.

Hydrogen-bonding abilities for phenols assessed by quantitative analyses of their partition coefficients derived from different partitioning systems.

We recently proposed a new hydrogen-accepting scale, S(HA), on the basis of the heat of formation calculated by the conductor-like screening model (COSMO) method. In this work, the same approach was applied to a series of compounds with a common hydrogen-donor group. Thus the S(HA) values for monosubstituted phenols were calculated and used for correlating their log P(oct) values (P(oct): 1-octanol/water partition coefficient) with log P(CL) (P(CL): chloroform/water partition coefficient) and log P(E) (P(E): butyl ether/water partition coefficient). It was demonstrated that the S(HA) parameter works effectively, providing excellent correlations whose physicochemical meanings are well rationalized in terms of hydrogen-bonding characteristics of the substituents.