公开(公告)号：US3760087A

公开(公告)日：1973-09-18

申请号：US3760087D

申请日：1970-01-19

Applicant: HOFFMANN LA ROCHE

Inventor： HAJOS Z ,  PARRISH D

IPC: A23L27/20 ,  C11B9/00 ,  C11D3/50 ,  C11D9/44 ,  A61K7/00

CPC classification number: C11D9/442 ,  A23L27/2024 ,  A23L27/2028 ,  C11B9/0019 ,  C11D3/50

Abstract: The present invention comprises perfume compositions containing ethyl 2,4-dioxohexanoate.

Abstract translation: 本发明包括含有2,4-二氧代己酸乙酯的香料组合物。

公开(公告)号：US3825569A

公开(公告)日：1974-07-23

申请号：US18011571

申请日：1971-09-13

Applicant: HOFFMANN LA ROCHE

Inventor： HAJOS Z ,  OLIVETO E

IPC: C07C43/12 ,  C07C45/00 ,  C07D309/12 ,  C07D317/16 ,  C07D317/26 ,  C07D13/04

CPC classification number: C07C45/69 ,  C07C43/12 ,  C07C45/00 ,  C07C45/64 ,  C07C45/71 ,  C07C2603/16 ,  C07C2603/26 ,  C07D309/12 ,  C07D317/16 ,  C07D317/26 ,  C07C49/16 ,  C07C49/753 ,  C07C49/513 ,  C07C49/633

Abstract: METHODS FOR THE PREPARATION OF 2,3,3A,4,5,7,8,9,9AB,9BADECAHYDRO - 3AB-PRIMARY LOWER ALKYL-7-OXO-1H-BENZ(E) INDENES AND 4,4AB,4BA,5,6,7,8,8A,9,10-DECAHYDRO-8AB-PRIMARY LOWER ALKYL - 3H-PHENANTHREN-2-ONES BY CYCLIZING COMPOUNDS OF THE FORMULA
WHERE R1 IS HYDROGEN OR LOWER ALKYL; Z'' IS CARBONYL OR CH(OR2''); R2'' IS HYDROGEN, LOWER AKYL, LOWER ALKANOYL, BENZOYL, NITROBENZOYL, CARBOXY-LOWER ALKANOYL, CARBOXYBENZOYL, TRIFLUOROACETYL OR CAMPHORSULFONYL; T'' IS -C(X'')=CH-, -C(OR3)=CH- OR -Q''-CH2-; R3 IS LOWER ALKYL; X'' IS BROMINE, CHLORINE OR IODINE; Q'' IS CARBONYL, LOWER ALKYLENE DIOXY-METHYLENE, DI-(LOWER ALKOXY)-METHYLENE OR HYDROXY-METHYLENE, R4 IS LOWER PRIMARY ALKYL AND M IS AN INTEGER HAVING A VALUE OF 1 OR 2. THE COMPOUNDS OF THIS SERIES ARE USEFUL AS INTERMEDIATES IN THE SYNTHESIS OF KNOWN STEROIDS WHICH ARE PHARMACOLOGICALLY ACTIVE AS FERTILITY CONTROL AGENTS.

CH3)-)

R1-CH2-T''-CH2-CH(-CO-H)-CH

公开(公告)号：US3852331A

公开(公告)日：1974-12-03

申请号：US29807072

申请日：1972-10-16

Applicant: HOFFMANN LA ROCHE

Inventor： HAJOS Z

IPC: C07C62/26 ,  C07C62/38 ,  C07C69/00

CPC classification number: C07C62/38 ,  C07C62/26 ,  C07C2603/16

Abstract: Total synthesis of known progestationally active steroidal materials. The steroids can be synthesized depending on the particular starting reactants selected by employing as intermediates bicyclic compounds of the formula

WHEREIN M IS AN INTEGER HAVING A VALUE OF 1 OR 2; R4 is hydrogen or lower alkyl; Z is lower alkylenedioxy, CH(OR2) and carbonyl; R8 when taken along is hydrogen; R9 when taken alone is lower alkoxycarbonyl, aryloxy-carbonyl, lower cycloalkyloxycarbonyl, carbonyl-halide, hydrogen, carboxy, formyl and methylene-X, where X is a leaving group and when taken together are methylene; with the proviso that when Z is carbonyl R8 when taken alone is hydrogen; R9 when taken alone is carbonyl halide, hydrogen, carboxy, formyl and methylene-X where X is a leaving group and when taken together are methylene and R2 is hydrogen, lower alkyl, lower alkoxy-lower alkyl, PHENYL-LOWER ALKYL, TETRAHYDROPYRANYL, LOWER ALKANOYL, BENZOYL, NITROBENZOYL, CARBOXY-LOWER ALKANOYL, CARBOXY-BENZOYL, TRIFLUOROACETYL AND CAMPHORSULFONYL AND REACTING THEM IN THE CASE WHERE R8 and R9 taken together are methylene or R8 is hydrogen and R9 is methylene-X with Beta keto esters and other analogs of the formula

WHEREIN R6 is selected from the group

LOWER ALKYL; R7 is lower alkyl; R15 is selected from the group consisting of oxo, lower alkylene-dioxy or (hydrogen and lower alkoxy); B is selected from the group consisting of lower alkoxycarbonyl-methylene, lower-aryloxy-carbonyl-methylene, cyanomethylene, lower alkyl sulfinyl-methylene, lower alkyl sulfonyl-methylene, and R25 and R26 are independently selected from the group consisting of hydrogen, hydroxyl and lower alkyl.

Abstract translation: 已知的促孕活性甾体材料的全合成。 可以根据通过使用作为中间体选择的特定起始反应物来合成类固醇，其具有下式的双环化合物，其中M是具有1或2的值的整数; R4是氢或低级烷基; Z是低亚烷基二氧基，CH（OR 2）和羰基; 取R8时为氢; 当单独使用时，R 9为低级烷氧基羰基，芳氧基羰基，低级环烷氧基羰基，羰基卤化物，氢，羧基，甲酰基和亚甲基-X，其中X为离去基团，并且一起为亚甲基时; 条件是当Z为羰基时，当单独使用时为氢; 当单独使用时，R 9是羰基卤，氢，羧基，甲酰基和亚甲基-X，其中X是离去基团，当它们一起是亚甲基且R 2是氢时，低级烷基，低级烷氧基 - 低级烷基，苯基 - 低级烷基，四氢呋喃基， 低级烷基，苯甲酰基，硝基苯甲酰，羧基 - 低级烷基，羧基 - 苯甲酰基，三氟乙酸和环戊二烯并在其中反应。其中R8和R9一起为亚甲基或R8为氢，R9为亚甲基-X，带有β-酮酯等 式WHERE R6的类似物选自LOWER ALKYL; R7是低级烷基; R 15选自氧代，低级亚烷基 - 二氧基或（氢和低级烷氧基）; B选自低级烷氧基 - 羰基 - 亚甲基，低级 - 芳氧基 - 羰基 - 亚甲基，氰基亚甲基，低级烷基亚磺酰基 - 亚甲基，低级烷基磺酰基 - 亚甲基，R 25和R 26独立地选自氢 ，羟基和低级烷基。

公开(公告)号：ZA7100020B

公开(公告)日：1971-10-27

申请号：ZA7100020

申请日：1971-01-04

Applicant: HOFFMANN LA ROCHE

Inventor： HAJOS Z ,  PARRISH D

IPC: C07C69/716 ,  C07C45/00 ,  C07C45/73 ,  C07C49/385 ,  C07C49/395 ,  C07C49/493 ,  C07C49/623 ,  C07C51/00 ,  C07C59/205 ,  C07C67/00 ,  C07D263/52 ,  C07D317/46 ,  C07D317/54 ,  C07D325/00

CPC classification number: C07D263/52 ,  C07C45/66 ,  C07C45/67 ,  C07C45/69 ,  C07C2603/16 ,  C07C49/633 ,  C07C49/513 ,  C07C49/753 ,  C07C49/395

公开(公告)号：SE331092B

公开(公告)日：1970-12-14

申请号：SE1392466

申请日：1966-10-13

Applicant: HOFFMANN LA ROCHE

Inventor： HAJOS Z ,  OLIVETO E

IPC: C07C49/643 ,  B01J23/00 ,  C07B61/00 ,  C07C45/00 ,  C07C45/60 ,  C07C49/16 ,  C07C49/737 ,  C07C49/755 ,  C07C67/00 ,  C07D309/12 ,  C07D317/16 ,  C07C49/54

公开(公告)号：SE365495B

公开(公告)日：1974-03-25

申请号：SE1363869

申请日：1969-10-03

Applicant: HOFFMANN LA ROCHE

Inventor： HAJOS Z

IPC: C07C225/12 ,  C07C49/513 ,  C07C49/557 ,  C07C49/613 ,  C07C49/653 ,  C07C49/753 ,  C07C61/13 ,  C07C62/18 ,  C07C62/24 ,  C07C62/26 ,  C07C62/38 ,  C07C67/00 ,  C07C225/00 ,  C07C233/12 ,  C07C301/00 ,  C07C303/28 ,  C07C309/65 ,  C07C317/00 ,  C07D317/26 ,  C07D317/30 ,  C07J1/00 ,  C07J75/00 ,  C07C49/36 ,  C07C49/38

公开(公告)号：BR6683552D0

公开(公告)日：1973-12-04

申请号：BR18355266

申请日：1966-10-11

Applicant: HOFFMANN LA ROCHE

Inventor： HAJOS Z ,  OLIVETO E

IPC: C07C49/643 ,  B01J23/00 ,  C07B61/00 ,  C07C45/00 ,  C07C45/60 ,  C07C49/16 ,  C07C49/737 ,  C07C49/755 ,  C07C67/00 ,  C07D309/12 ,  C07D317/16

公开(公告)号：SE365196B

公开(公告)日：1974-03-18

申请号：SE1363769

申请日：1969-10-03

Applicant: HOFFMANN LA ROCHE

Inventor： HAJOS Z

IPC: C07C225/12 ,  C07C49/513 ,  C07C49/557 ,  C07C49/613 ,  C07C49/653 ,  C07C49/753 ,  C07C61/13 ,  C07C62/18 ,  C07C62/24 ,  C07C62/26 ,  C07C62/38 ,  C07C67/00 ,  C07C225/00 ,  C07C233/12 ,  C07C301/00 ,  C07C303/28 ,  C07C309/65 ,  C07C317/00 ,  C07D317/26 ,  C07D317/30 ,  C07J1/00 ,  C07J75/00 ,  C07C49/36 ,  C07C49/38

公开(公告)号：CA937871A

公开(公告)日：1973-12-04

申请号：CA103046

申请日：1971-01-19

Applicant: HOFFMANN LA ROCHE

Inventor： HAJOS Z ,  PARRISH D

IPC: A61K20060101

公开(公告)号：PH12661A

公开(公告)日：1979-07-11

申请号：PH12122

申请日：1971-01-10

Applicant: HOFFMANN LA ROCHE

Inventor： HAJOS Z ,  PARRISH D

IPC: C07C69/716 ,  C07C20060101 ,  C07C45/00 ,  C07C45/73 ,  C07C49/385 ,  C07C49/395 ,  C07C49/493 ,  C07C49/623 ,  C07C51/00 ,  C07C59/205 ,  C07C67/00 ,  C07D263/52 ,  C07D317/46 ,  C07D317/54 ,  C07D325/00 ,  C07J1/00 ,  C07C49/00

Abstract: Optically active organic compounds are prepared starting from optically inactive reactants by means of an optically active agent which influences the course of the reaction. In particular optically active compounds having a "meso" type carbon atom undergo an intramolecular ring closure in the presence of an optically active agent to yield an optically active product having one additional ring. The present process is particularly useful in the preparation of optically active bicyclic diketones which are important intermediates in the total synthesis of steroids.