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    PRODUCTION OF ORTHOCARBONIC ACID ESTERS
    31.
    发明专利
    PRODUCTION OF ORTHOCARBONIC ACID ESTERS 失效

    公开(公告)号：JPH10245365A

    公开(公告)日：1998-09-14

    申请号：JP4879797

    申请日：1997-03-04

    Applicant: AGENCY IND SCIENCE TECHN

    Inventor： SHIBUYA ISAO ,  GAMA YASUO ,  SHIMIZU MASAO

    IPC: C07D493/10 ,  C07C41/60 ,  C07C43/32 ,  C07C68/00 ,  C07C69/96

    Abstract: PROBLEM TO BE SOLVED: To safely produce the subject compounds useful as an intermediate for agrochemical, medicines, etc., in high yield without using a special raw material by carrying out the desulfurizing reaction of a mono- and a dihydroxy compound and carbon disulfide in the presence of a base and a heavy metallic compound. SOLUTION: The desulfurizing reaction of (A) a monohydroxy compound represented by the formula R -OH (R is a monovalent hydrocarbon group, etc.) (e.g. ethanol) or (B) a dihydroxy compound represented by the formula HO-R -OH (R is a bivalent hydrocarbon group, etc.) (e.g. catechol) is carried out in the presence of a base (e.g. a tertianry amine such as triethylamine) and a heavy metallic compound (e.g. silver trifluoroacetate) to thereby afford the objective compound represented by formula I from the compound A or the objective compound represented by formula II from the compound B. A solvent (e.g. acetonitrile) is advantageously used for the desulfurizing reaction. The objective compound is useful as a synthetic intermediate for, e.g. guanidines, esters, carboxylic acid orthoesters, heterocyclic compounds etc., and used as an intermediate raw material for agrochemical, medicines and other organic chemicals.

    LIPOSOME
    33.
    发明专利
    LIPOSOME 失效

    公开(公告)号：JPH0474116A

    公开(公告)日：1992-03-09

    申请号：JP18848590

    申请日：1990-07-16

    Applicant: AGENCY IND SCIENCE TECHN ,  LINTEC CORP

    Inventor： GAMA YASUO ,  ISHIGAMI YUTAKA ,  OKABE HIDEAKI ,  KAMAGAMI SABURO ,  KAIZE HISAYASU

    IPC: A61K8/30 ,  A61K8/11 ,  A61K8/14 ,  A61K8/44 ,  A61K9/127

    Abstract: PURPOSE:To obtain a liposome capable of releasing included drug according to the reducting condition and pH condition of outer aqueous phase and having excellent affinity to keratin by including N,N'-diacylcystine in wall membrane. CONSTITUTION:The wall membrane material of the objective lipsome is composed of a mixture of phospholipid molecule and N,N'-diacylcystine and, as necessary, added with cholesterol to reinforce a bimolecular membrane and dicetyl phosphate,stearylamine, etc., as a charge substance. The acyl group of the N,N'-diacylcystine has a C-number of 8-22, preferably 10-18 and the amount of the diacylcystine is 5-40 mol%, preferably 10-30 mol% based on total wall membrane. When the above liposome containing insulin as a drug component is administered, glucose is dehydrogenated with enzyme in the body activated by the increase of glucose and, as a result, cystine is reduced and insulin is released by the destruction of liposome. Accordingly, the objective liposome is useful as a remedy for diabetes.

    1,8-BIS(2-MERCAPTOETHYL)NAPHTHALENE, ITS DERIVATIVE AND PRODUCTION
    34.
    发明专利
    1,8-BIS(2-MERCAPTOETHYL)NAPHTHALENE, ITS DERIVATIVE AND PRODUCTION 失效

    公开(公告)号：JPH0341064A

    公开(公告)日：1991-02-21

    申请号：JP17533989

    申请日：1989-07-06

    Applicant: AGENCY IND SCIENCE TECHN

    Inventor： KAMATA TOSHIHIRO ,  GAMA YASUO ,  WASADA NOBUHIDE

    IPC: C07C327/22 ,  C07C319/02 ,  C07C321/10

    Abstract: NEW MATERIAL:1,8-Bis(2-Mercaptoethyl)naphthalane expressed by formula I. USE:A monomer for polysulfides or polythioesters or raw material for producing surfactants or heavy metal capturing agents. PREPARATION:A 1,8-bis(2-halogenoethyl)naphthalene expressed by formula II (X is halogen) is heat-treated with thiourea in an alcohol and then thermally refluxed with an alkaline aqueous solution in N2 atmosphere to produce a compound expressed by formula III (M is alkali metal), which is subsequently treated with an acid to afford the compound expressed by formula I. The resultant compound is further reacted with an acylating agent to provide a 1,8-bis(2- mercaptoethyl)naphthalene derivative expressed by formula IV (R is acyl) which is a novel compound.

    1,8-BIS(2-HALOGENOETHYL)NAPHTHALENE AND PRODUCTION THEREOF
    36.
    发明专利
    1,8-BIS(2-HALOGENOETHYL)NAPHTHALENE AND PRODUCTION THEREOF 失效

    公开(公告)号：JPH02258734A

    公开(公告)日：1990-10-19

    申请号：JP7932989

    申请日：1989-03-30

    Applicant: AGENCY IND SCIENCE TECHN

    Inventor： KAMATA TOSHIHIRO ,  GAMA YASUO ,  WASADA NOBUHIDE

    IPC: C07C17/16 ,  C07C17/20 ,  C07C22/02 ,  C07C22/04

    Abstract: NEW MATERIAL:The 1, 8-bis(2-halogenoethyl)naphthalene of formula I (X is Br or Cl). EXAMPLE:1,8-Bis(2-bromoethyl)naphthalene. USE:Raw material for the production of a monomer for polyester or polyether or a surfactant. PREPARATION:The compound of formula I can be produced by subjecting 1,8-divinylnaphthalene of formula II to hydroboration reaction with bis(3- methyl-2-butyl)borane and reacting the resultant 1,8-bis(2-hydroxyethyl) naphthalene of formula III with a halogenation agent such as hydrobromic acid at room temperature to 80 deg.C. As an alternative method, a compound of formula I wherein X is Cl is produced by reacting a new 1,8-bis(2-bromoethyl) naphthalene of formula IV with a halogen exchange agent such as LiCl in a solvent (e. g. N,N'-dimethylformamide) at room temperature to 50 deg.C for 3-6 days.

    SULFENAMIDE COMPOUND AND ITS PRODUCTION
    38.
    发明专利
    SULFENAMIDE COMPOUND AND ITS PRODUCTION 失效

    公开(公告)号：JP2000095751A

    公开(公告)日：2000-04-04

    申请号：JP28339298

    申请日：1998-09-18

    Applicant: AGENCY IND SCIENCE TECHN ,  SHIMIZU MASAO ,  SHIBUYA ISAO

    Inventor： SHIMIZU MASAO ,  SHIBUYA ISAO ,  GAMA YASUO

    IPC: C07C313/24 ,  C07D275/04

    Abstract: PROBLEM TO BE SOLVED: To obtain a new sulfenamide useful for profitably producing benzoisothiazolinone compounds by aminating the thiol group of a thiosalicylic acid ester compound without using a poisonous chlorine gas and a starting raw material which is difficult to obtain. SOLUTION: A compound of formula I [R1-R4 are each H or an inactive substituent (for example, an alkyl group); R5 is an inactive ingredient (for example, an aliphatic group)]. For example, a compound of formula II. The compound of formula I is obtained by aminating a thiosalicylic acid ester compound of formula III. The amination reaction is preferably carried out by reacting 1 equivalent of the thiosalicylic acid ester with 1.0-3 equivalents of the aminating agent (for example, hydroxyamine-O-sulfonic acid) in a reaction solvent (for example, water, a 1-6C aliphatic alcohol such as methanol, an ether compound such as diethyl ether or a nitrogen-containing organic solvent such as acetonitrile) at -30 to 50 deg.C.

    RHAMNOLIPID PYRENACYL ESTER
    39.
    发明专利
    RHAMNOLIPID PYRENACYL ESTER 失效

    公开(公告)号：JPH01283295A

    公开(公告)日：1989-11-14

    申请号：JP11116988

    申请日：1988-05-06

    Applicant: AGENCY IND SCIENCE TECHN

    Inventor： GAMA YASUO ,  ISHIGAMI YUTAKA

    IPC: C07H15/04 ,  C09K11/06

    Abstract: NEW MATERIAL:(2-O-alpha-decenoyl-alpha-L-rhamnopyranocyl-beta-hydroxydecan oyl-beta- hydroxydecanoic acid)-pyrenacyl ester expressed by the formula. USE:The aimed material is a fluorescent material of glucolipid type and useful for fluorescent probe material and research of biomembrane or liposome. PREPARATION:For instance, potassium salt or sodium salt of rhamnolipid and 1-bromoacetylpyrene are subjected to desalting reaction in hydrous alcohol or hydrous acetonitrile.

    POLYBASIC ACID POLYETHER DERIVATIVE AND SURFACTANT COMPRISING SAME
    40.
    发明专利
    POLYBASIC ACID POLYETHER DERIVATIVE AND SURFACTANT COMPRISING SAME 失效

    公开(公告)号：JPS63112622A

    公开(公告)日：1988-05-17

    申请号：JP25949486

    申请日：1986-10-30

    Applicant: AGENCY IND SCIENCE TECHN

    Inventor： SUZUKI HIROSHI ,  MIYAZAKI SHOJI ,  GAMA YASUO ,  SUHARA YASUO

    IPC: B01F17/00 ,  B01F17/42 ,  B01F17/52 ,  C08G65/32 ,  C09K3/16 ,  C11D1/08

    Abstract: PURPOSE:To obtain the title derivative useful as a surfactant excellent in emulsifying power, dispersing power, chelating power, surface tension depressing power, corrosion-inhibiting power, antibacterial activity, etc., having a specified structural formula. CONSTITUTION:A cyclohexene ring-containing aliphatic derivative of formula I or II (wherein R and R' are each H or an alkyl) and glacial acetic acid are ozonized at 10-14 deg.C in the presence of an ozone/oxygen mixture, and the formed ozonide is decomposed and then oxidized to obtain a compound (a), which is an acid or a partial alkyl ester, of formula III (wherein n and n' are each 4-15, Y is H or COOR and R is H or a 1-18C alkyl, provided that at least one of them is H). Component (a) is esterified with a polyalkylene glycol (b) (PAG) of a degree of polymerization of 1-20 and the product is neutralized or saponified to obtain a tetra- or penta-carboxylic acid derivative of formula IV [wherein X is H or COOA, A is a PAG residue of formula V (wherein m is 2-4 and p is 1-20), H, a 1-18C alkyl, an alkali metal, or an (alkanol) ammonium ion, and at least one X is a PAG residue].

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